- Young Chemists who have just started work in industry as development chemists
- Organic Chemists/Medicinal Chemists in Research and Development who would like to gain an appreciation of development and scale up and who are perhaps contemplating moving into chemical development.
- Development and Production Chemists in industry who would like to improve their efficiency and gain an insight into alternative approaches to chemical development.
- Chemical Engineers who wish to understand a chemist’s approach to chemical development of batch processes. (Engineers would, however, need a good grounding in organic chemistry)
- Students who are about to enter the industry and can obtain company sponsorship.
- Experienced Chemists looking to refresh and/or augment their knowledge of chemical development
- Analytical Chemists who wish to gain a broader appreciation of process chemistry
- Managers who might benefit from a comprehensive and up to date overview of chemical development
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Dr Will Watson, an expert in Chemical Development and related fields, from Scientific Update will be visiting India in February to deliver two important workshops for Industrial Process Chemists:
Chemical Development and Scale Up in the Fine Chemical and Pharmaceutical Industries, February 5th – 7th 2018, Hyderabad, India
Practical Crystallisation & Polymorphism, February 8th & 9th 2018, Hyderabad, India
Discounts are available for groups – please contact email@example.com for more information.
Lifetime achievement award ……..WORLD HEALTH CONGRESS 2017 in Hyderabad, 22 aug 2017 at JNTUH KUKATPALLY. HYDERABAD, TELANGANA, INDIA, Award given by Dr. M Sunitha Reddy Head of the Department, Centre for Pharmaceutical Sciences, Institute of Science &Technology, JNTU-H, Kukatpally, Hyderabad, India
Speaking at World health congress 2017….JNTUH Hyderabad 22 aug 2017
Register Today for the ACS Symposium in India on Recent Advances in Drug Development, 11-12 November 2016 in Hyderabad, India
Inaugural ACS Industry Symposium, 11-12 November 2016 in Hyderabad, India
Recent Advances in Drug Development
Register Today for the ACS Symposium in India on Recent Advances in Drug Development
To view this email as a web page, go here.
Register now for the inaugural ACS Industry Symposium, 11-12 November 2016 in Hyderabad, India. Be sure to secure your seat today as rates will increase on 27 October!
The theme of the Symposium is Recent Advances in Drug Development. The event will feature lectures by the world’s leading researchers and experts in the pharma industry, including:
- Dr. Peter Senter of Seattle Genetics
- Dr. Jagath Reddy Junutula of Cellerant Therapeutics, Inc.
- Dr. Ming-Wei Wang of the Shanghai Institute of Materia Medica, Chinese Academy of Sciences
This is an exclusive event being organized in partnership with Dr. Reddy’s Laboratories for pharma professionals throughout India. Space is limited so register today!
Please visit our website to learn more about the speakers and the program.
Register today to ensure your access to the ACS Industry Symposium. We look forward to seeing you in Hyderabad in November.
2540 Olentangy River Rd Columbus, OH 43202 US
2540 Olentangy River Rd Columbus, OH 43202 US
Inaugural ACS Industry Symposium, 11-12 November 2016 in Hyderabad, India
Recent Advances in Drug Development
/////// ACS Symposium, Recent Advances in Drug Development, 11-12 November 2016, Hyderabad, India, dr reddys, cas
Sreeni Labs Private Limited, Hyderabad, India ready to deliver New, Economical, Scalable Routes to your advanced intermediates & API’s in early Clinical Drug Development Stages
Sreeni Labs Private Limited, Hyderabad, India is ready to take up challenging synthesis projects from your preclinical and clinical development and supply from few grams to multi-kilo quantities. Sreeni Labs has proven route scouting ability to design and develop innovative, cost effective, scalable routes by using readily available and inexpensive starting materials. The selected route will be further developed into a robust process and demonstrate on kilo gram scale and produce 100’s of kilos of in a relatively short time.
Accelerate your early development at competitive price by taking your route selection, process development and material supply challenges (gram scale to kilogram scale) to Sreeni Labs…………
Sreeni Labs based in Hyderabad, India is working with various global customers and solving variety of challenging synthesis problems. Their customer base ranges from USA, Canada, India and Europe. Sreeni labs Managing Director, Dr. Sreenivasa Reddy Mundla has worked at Procter & Gamble Pharmaceuticals and Eli Lilly based in USA.
The main strength of Sreeni Labs is in the design, development of innovative and highly economical synthetic routes and development of a selected route into a robust process followed by production of quality product from 100 grams to 100s of kg scale. Sreeni Labs main motto is adding value in everything they do.
They have helped number of customers from virtual biotech, big pharma, specialty chemicals, catalog companies, and academic researchers and drug developers, solar energy researchers at universities and institutions by successfully developing highly economical and simple chemistry routes to number of products that were made either by very lengthy synthetic routes or by using highly dangerous reagents and Suzuki coupling steps. They are able to supply materials from gram scale to multi kilo scale in a relatively short time by developing very short and efficient synthetic routes to a number of advanced intermediates, specialty chemicals, APIs and reference compounds. They also helped customers by drastically reducing number of steps, telescoping few steps into a single pot. For some projects, Sreeni Labs was able to develop simple chemistry and avoided use of palladium & expensive ligands. They always begin the project with end in the mind and design simple chemistry and also use readily available or easy to prepare starting materials in their design of synthetic routes
Over the years, Sreeni labs has successfully made a variety of products ranging from few mg to several kilogram scale. Sreeni labs has plenty of experience in making small select libraries of compounds, carbocyclic compounds like complex terpenoids, retinal derivatives, alkaloids, and heterocyclic compounds like multi substituted beta carbolines, pyridines, quinolines, quinolones, imidazoles, aminoimidazoles, quinoxalines, indoles, benzimidazoles, thiazoles, oxazoles, isoxazoles, carbazoles, benzothiazoles, azapines, benzazpines, natural and unnatural aminoacids, tetrapeptides, substituted oligomers of thiophenes and fused thiophenes, RAFT reagents, isocyanates, variety of ligands, heteroaryl, biaryl, triaryl compounds, process impurities and metabolites.
Sreeni Labs is Looking for any potential opportunities where people need development of cost effective scalable routes followed by quick scale up to produce quality products in the pharmaceutical & specialty chemicals area. They can also take up custom synthesis and scale up of medchem analogues and building blocks. They have flexible business model that will be in sink with customers. One can test their abilities & capabilities by giving couple of PO based (fee for service) projects.
Some of the compounds prepared by Sreeni labs;
See presentation below
LINK ON SLIDESHARE
Managing Director at Sreeni Labs Private Limited\
Few Case Studies : Source SEEENI LABS
One virtual biotech company customer from USA, through a common friend approached Sreeni Labs and told that they are buying a tetrapeptide from Bachem on mg scale at a very high price and requested us to see if we can make 5g. We accepted the challenge and developed solution phase chemistry and delivered 6g and also the process procedures in 10 weeks time. The customer told that they are using same procedures with very minor modifications and produced the tetrapeptide ip to 100kg scale as the molecule is in Phase III.
One East coast customer in our first meeting told that they are working with 4 CROs of which two are in India and two are in China and politely asked why they should work with Sreeni Labs. We told that give us a project where your CROs failed to deliver and we will give a quote and work on it. You pay us only if we deliver and you satisfy with the data. They immediately gave us a project to make 1.5g and we delivered 2g product in 9 weeks. After receiving product and the data, the customer was extremely happy as their previous CRO couldn’t deliver even a milligram in four months with 3 FTEs.
One Midwest biotech company was struggling to remove palladium from final API as they were doing a Suzuki coupling with a very expensive aryl pinacol borane and bromo pyridine derivative with an expensive ligand and relatively large amount of palldium acetate. The cost of final step catalyst, ligand and the palladium scavenging resin were making the project not viable even though the product is generating excellent data in the clinic. At this point we signed an FTE agreement with them and in four months time, we were able to design and develop a non suzuki route based on acid base chemistry and made 15g of API and compared the analytical data and purity with the Suzuki route API. This solved all three problems and the customer was very pleased with the outcome.
One big pharma customer from east coast, wrote a structure of chemical intermediate on a paper napkin in our first meeting and asked us to see if we can make it. We told that we can make it and in less than 3 weeks time we made a gram sample and shared the analytical data. The customer was very pleased and asked us to make 500g. We delivered in 4 weeks and in the next three months we supplied 25kg of the same product.
Through a common friend reference, a European customer from a an academic institute, sent us an email requesting us to quote for 20mg of a compound with compound number mentioned in J. med. chem. paper. It is a polycyclic compound with four contiguous stereogenic centers. We gave a quote and delivered 35 mg of product with full analytical data which was more pure than the published in literature. Later on we made 8g and 6g of the same product.
One West coast customer approached us through a common friend’s reference and told that they need to improve the chemistry of an advanced intermediate for their next campaign. At that time they are planning to make 15kg of that intermediate and purchased 50kg of starting raw material for $250,000. They also put five FTEs at a CRO for 5 months to optimize the remaining 5 steps wherein they are using LAH, Sodium azide, palladium catalyst and a column chromatography. We requested the customer not to purchase the 50kg raw material, and offered that we will make the 15kg for the price of raw material through a new route in less than three months time. You pay us only after we deliver 15 kg material. The customer didn’t want to take a chance with their timeline as they didn’t work with us before but requested us to develop the chemistry. In 7 weeks time, we developed a very simple four step route for their advanced intermediate and made 50g. We used very inexpensive and readily available starting material. Our route gave three solid intermediates and completely eliminated chromatographic purifications.
One of my former colleague introduced an academic group in midwest and brought us a medchem project requiring synthesis of 65 challenging polyene compounds on 100mg scale. We designed synthetic routes and successfully prepared 60 compounds in a 15 month time.
The man behind Seeni labs is Dr. Sreenivasa Reddy Mundla
Dr. Sreenivasa Reddy Mundla.
Managing Director at Sreeni Labs Private Limited
Sreeni Labs Private Limited
Road No:12, Plot No:24,25,26
- IDA, Nacharam
Telangana State, India
Dr. Sreenivasa Reddy Mundla
Dr. M. Sreenivasa Reddy obtained Ph.D from University of Hyderabad under the direction Prof Professor Goverdhan Mehta in 1992. From 1992-1994, he was a post doctoral fellow at University of Wisconsin in Professor Jame Cook’s lab. From 1994 to 2000, worked at Chemical process R&D at Procter & Gamble Pharmaceuticals (P&G). From 2001 to 2007 worked at Global Chemical Process R&D at Eli Lilly and Company in Indianapolis.
In 2007 resigned to his job and founded Sreeni Labs based in Hyderabad, Telangana, India and started working with various global customers and solving various challenging synthesis problems.
The main strength of Sreeni Labs is in the design, development of a novel chemical route and its development into a robust process followed by production of quality product from 100 grams to 100’s of kg scale.
They have helped number of customers by successfully developing highly economical simple chemistry routes to number of products that were made by Suzuki coupling. they are able to shorten the route by drastically reducing number of steps, avoiding use of palladium & expensive ligands. they always use readily available or easy to prepare starting materials in their design of synthetic routes.
Sreeni Labs is Looking for any potential opportunities where people need development of cost effective scalable routes followed by quick scale up to produce quality products in the pharmaceutical & specialty chemicals area. They have flexible business model that will be in sink with customers. One can test their abilities & capabilities by giving PO based projects
August 2007 – Present (8 years 11 months)
March 2001 – August 2007 (6 years 6 months)
July 1994 – February 2001 (6 years 8 months)
Aug 2010 · ChemInform
Article: Optimization of a Dihydropyrrolopyrazole Series of Transforming Growth Factor-β Type I Receptor Kinase Domain Inhibitors: Discovery of an Orally Bioavailable Transforming Growth Factor-β Receptor Type I Inhibitor as Antitumor Agent
Hong-yu Li · William T. McMillen · Charles R. Heap · Denis J. McCann · Lei Yan · Robert M. Campbell · Sreenivasa R. Mundla · Chi-Hsin R. King · Elizabeth A. Dierks · Bryan D. Anderson · Karen S. Britt · Karen L. Huss
Apr 2008 · Journal of Medicinal Chemistry
Feb 2008 · ChemInform
Nov 2007 · Tetrahedron
Article: Dihydropyrrolopyrazole Transforming Growth Factor-β Type I Receptor Kinase Domain Inhibitors: A Novel Benzimidazole Series with Selectivity versus Transforming Growth Factor-β Type II Receptor Kinase and Mixed Lineage Kinase-7
Hong-yu Li · Yan Wang · Charles R Heap · Chi-Hsin R King · Sreenivasa R Mundla · Matthew Voss · David K Clawson · Lei Yan · Robert M Campbell · Bryan D Anderson · Jill R Wagner ·Karen Britt · Ku X Lu · William T McMillen · Jonathan M Yingling
Apr 2006 · Journal of Medicinal Chemistry
Aug 2003 · Tetrahedron Letters
Nov 2000 · ChemInform
Nov 2000 · ChemInformAug 2000 · Tetrahedron LettersAug 2000 · Tetrahedron LettersArticle: Synthesis and Evaluation of Analogues of the Partial Agonist 6-(Propyloxy)-4-(methoxymethyl)-β-carboline-3-carboxylic Acid Ethyl Ester (6-PBC) and the Full Agonist 6-(Benzyloxy)-4-(methoxymethyl)-β- carboline-3-carboxylic Acid Ethyl Ester (Zk 93423) at Wild Type and Recombinant GABA A Receptors
The present invention provides 2-(6-methyl-pyridin-2-yl)-3-[6-amido-quinolin-4-yl) -5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole monohydrate, i.e., Formula I.
EXAMPLE 1 Preparation of 2-(6-methyl-pyridin-2-yl)-3-[6-amido-quinolin-4-yl-5,6-dihydro-4H -pyrrolo[1,2-b]pyrazole monohydrate
1H NMR (CDCl3): δ=9.0 ppm (d, 4.4 Hz, 1H); 8.23-8.19 ppm (m, 2H); 8.315 ppm (dd, 1.9 Hz, 8.9 Hz, 1H); 7.455 ppm (d, 4.4 Hz, 1H); 7.364 ppm (t, 7.7 Hz, 1H); 7.086 ppm (d, 8.0 Hz, 1H); 6.969 ppm (d, 7.7 Hz, 1H); 6.022 ppm (m, 1H); 5.497 ppm (m, 1H); 4.419 ppm (t, 7.3 Hz, 2H); 2.999 ppm (m, 2H); 2.770 ppm (p, 7.2 Hz, 7.4 Hz, 2H); 2.306 ppm (s, 3H); 1.817 ppm (m, 2H). MS ES+: 370.2; Exact: 369.16
ABOVE MOLECULE IS
A TGF-beta receptor type-1 inhibitor potentially for the treatment of myelodysplastic syndrome (MDS) and solid tumours.
READ MY PRESENTATION ON
KEYWORDS Sreenivasa Mundla Reddy, Managing Director, Sreeni Labs Private Limited, Hyderabad, Telangana, India, new, economical, scalable routes, early clinical drug development stages, Custom synthesis, custom manufacturing, drug discovery, PHASE 1, PHASE 2, PHASE 3, API, drugs, medicines
MESSAGE FROM VIJAY KIRPALANI
A 2-day FLOW CHEMISTRY Symposium + Workshop has been organized on 16-17 June 2016 at
IICT Hyderabad, India by Flow Chemistry Society – India Chapter (in collaboration with IICT-Hyderabad & IIT-B)
with speakers from India, UK, Netherlands and Hungary.
Both days have intensive interactive sessions on the theory and industrial applications of Flow Chemistry followed by live demonstrations using 7 different Flow Reactor platforms — from microliters to 10,000 L/day industrial scale.
I have attached a detailed program and look forward to meeting you at the event..
Flow Chemistry Society – India Chapter
email : firstname.lastname@example.org
Tel: +91-9321342022 // +91-9821342022
IICT, Hyderabad, India
Dr. S. Chandrasekhar,
CSIR-Indian Institute of Chemical Technology (IICT)
Mr Vijay Kirpalani
Flow Chemistry Society – India Chapter, INDIA
Dr Charlotte Wiles , CHEMTRIX
UK &THE NETHERLANDS,UNIV OF HULL
Prof Anil Kumar( IIT-B), INDIA
/////Flow Chemistry, Symposium, Workshop, 16-17 June, IICT, Hyderabad, India
WO2016012938, IMPROVED PROCESS FOR PREPARATION OF AMORPHOUS LINACLOTIDE
DR. REDDY’S LABORATORIES LIMITED [IN/IN]; 8-2-337, Road No 3, Banjara Hills, Telangana, INDIA Hyderabad 500034 (IN)
KALITA, Dipak; (IN).
NIVRUTTI, Ramrao Jogdand; (IN).
BALAKUMARAN, Kesavan; (IN).
DESHMUKH, Shivshankar; (IN).
VUTUKURU, Naga Chandra Sekhar; (IN).
KASINA, Vara Prasad; (IN).
NALAMOTHU, Sivannarayana; (IN).
VILVA, Mohan Sundaram; (IN).
KHAN, Rashid Abdul Rehman; (IN).
TIRUMALAREDDY, Ramreddy; (IN).
MUSTOORI, Sairam; (IN)
The present application relates to an improved process for the formation of disulfide bonds in linaclotide. The present application also relates to an improved process for the purification of linaclotide.
The present application relates to an improved process for the preparation of amorphous linaclotide. Specifically, the present application relates to an improved process for the formation of disulfide bonds in linaclotide. The present application further relates to a purification process for the preparation of amorphous linaclotide.
Linaclotide is a 14-residue peptide which is an agonist of the guanylate cyclase type-C receptor. Linaclotide may be used for the treatment of chronic constipation and irritable bowel syndrome. Structurally, linaclotide has three disulfide bonds and they are present between Cys1-Cys6, Cys2-Cys-10 and Cys5-Cys13. The structure of linaclotide is shown below:
1 2 3 4 5 6 7 8- 9 10 11 12 13 14
Benitez et al. Peptide Science, 2010, Vol. 96, No. 1 , 69-80 discloses a process for the preparation of linaclotide. The process involves the use of 2-chlorotrityl (CTC) resin and 9-fluorenylmethoxycarbonyl (Fmoc) chemistry. The Cys residues are protected by Trt (trityl) group. The amino acids are coupled to one another using 3 equivalents of 1 -[bis(dimethylamino)methylene]-6-chloro-1 H-benzotriazolium hexafluorophosphate 3-oxide (HCTU) as coupling agent and 6 equivalents of diisoprpylethylamine (DIEA) as base in dimethylformamide (DMF). The Fmoc group is removed using piperidine-DMF (1 :4). The Cys residues are incorporated using 3 equivalents of Ν,Ν’-diisopropylcarbodiimide (DIPCDI) as coupling agent and 3 equivalents of 1 -hydroxybenzotriazole (HOBt) as an activating agent. After the elongation of the peptide chain, the peptide was cleaved from the solid support (CTC resin) by first treating with 1 % trifluoroacetic acid (TFA) and then with a mixture of TFA, triisoprpylsilane (TIS) and water in the ratio of 95:2.5:2.5. The disulfide bonds are prepared by subjecting the linear peptide to air oxidation in sodium dihydrogen phosphate (100 mM) and guanidine hydrochloride buffer (2 mM).
US2010/261877A1 discloses a process for purification of linaclotide. The process involves first purification of crude peptide by reverse-phase chromatographic purification followed by concentrating the purified pools and dissolving the purified linaclotide in aqueous-isopropanol or aqueous-ethanol and spray-drying the solution to afford pure Linaclotide.
The synthesis of a peptide containing disulfide bridges is difficult for two main reasons; one is potential risk of racemization during the formation of linear chain and the other is mis-folding of the disulfide bridges. Hence, there is a need in the art to a cost-effective process for the preparation of pure linaclotide.
Example 1 : Preparation of Crude Linaclotide using polyvinyl polymer bound complex of sulfur trioxide-pyridine
The linear chain of peptide of formula (I) (0.1 g) and polyvinyl polymer bound complex of sulfur trioxide-pyridine (0.062 g) was charged in water (100 mL). The pH of the reaction mass was adjusted to 8.5 to 9 by addition of ammonium hydroxide. The reaction mass was stirred at 25 °C for 15 hours and trifluoroacetic acid (2 mL) was added to the reaction mass to adjust the pH up to 2-2.5. The reaction mass was stirred for 3 hours at the same temperature to afford crude linaclotide.
HPLC Purity: 59.92%
Example 2: Preparation of Crude Linaclotide using DMSO in water
The pH of water (100 ml_) was adjusted to 9.1 by the addition of aqueous ammonia. DMSO (1 ml_) and linear chain of peptide of formula (I) (100 mg) were charged. The reaction mass was stirred for 17 hours at 25 °C and acidified with trifluoroacetic acid to pH 1 .9 and stirred for 8 hours at the same temperature to afford crude linaclotide.
HPLC Purity: 57%
Example 3: Preparation of Crude Linaclotide using DMSO in water
The pH of water (1500 ml_) was adjusted to 9 by the addition of aqueous ammonia. DMSO (15 ml_) and linear chain of peptide of formula (I) (15 g) were charged. The reaction mass was stirred for 17 hours at 25 °C and acidified with acetic acid to pH 1 .9 and stirred for 8 hours at the same temperature to obtain crude linaclotide.
HPLC Purity: 46.02%
Example 4: Preparation of Crude Linaclotide in water
To a mixture of water (1900 mL) and ammonium sulfate (26.4 g), ammonium hydroxide was added drop wise to adjust the pH up to 8.5. Linear chain of peptide of formula (I) (26.4 g) was added and the reaction mass was stirred for 8 hours at 25 °C. Trifluoroacetic acid (20 mL) was added drop wise and the reaction mixture was stirred for 15 hours at 25 °C to afford crude linaclotide.
HPLC Purity: 63.38%
Example 5: Preparation of Crude Linaclotide using a complex of pyridine-sulfur trioxide
Linear chain of peptide of formula (I) (0.2 g) was added to water (250 mL) and the pH of the reaction mass was adjusted to 8.91 by the drop wise addition of aqueous ammonia. A complex of pyridine-sulfur trioxide (0.124 g) was added to the reaction mass and stirred for 16 hours at 25 °C. Another lot of complex of pyridine-sulfur trioxide (0.124 g) was added to the reaction mass and stirred for 5 hours at 25 °C to afford crude linaclotide.
Example 6: Preparation of Crude Linaclotide using guanidine hydrochloride
To a solution of sodium bicarbonate (0.89 g) in water (100 mL), cysteine (0.363 g), cysteine (0.072 g) and guanidine hydrochloride (9.50 g) were charged. Acetonitrile (15 mL) and linear chain of peptide of formula (I) (0.1 g) was added to the reaction mass.
The reaction mass was stirred for 3 hours at 25 °C and trifluoroacetic acid (2 mL) was added. The reaction mass was stirred for 18 hours at the same temperature. Another lot of trifluoroacetic acid (2 mL) was added to the reaction mass and stirred for 18 hours at the same temperature to afford crude linaclotide.
Example 7: Preparation of Crude Linaclotide using Clear-OX™
Pre-conditioned Clear-Ox™ (0.5 g) was added to a solution of ammonium sulfate (1 .32 g) in water (100 mL) of pH 8.5, adjusted by addition of ammonium hydroxide. The linear chain of peptide of formula (I) (0.1 g) was added to the reaction mass and stirred for 3 hours at 25 °C. Another lot of Pre-conditioned Clear-Ox™ (0.5 g) was added to the reaction mass and stirred for 1 .30 hours. Trifluoroacetic acid (2 mL) was added to the reaction mass and stirred for 16 hours at the same temperature to afford crude linaclotide.
HPLC Purity: 67.5%
Example 8: Preparation of Crude Linaclotide using reduced Glutathione
To a mixture of ammonium sulphate (5.28 g) in water (400 mL) and isopropyl alcohol (400 mL), reduced glutathione (0.248 g) was added and the pH was adjusted to 8.5 by using aqueous ammonia. The linear chain of peptide of formula (I) (0.81 g) was added to the reaction mixture and stirred at ambient temperature for 17 hours. Isopropyl alcohol was evaporated under vacuum to afford crude linaclotide.
HPLC Purity: 69.56%%
Example 9: Preparation of Crude Linaclotide using DMSO and air bubbling
To a mixture of water (95 mL) and ammonium sulfate (1 .32 g), ammonium hydroxide was added drop wise to adjust the pH up to 8.5. Linear chain of peptide of formula (I) (0.1 g) and DMSO (5 mL) was added and the reaction mass was stirred for 20 hours at 25 °C with continuous air bubbling. Trifluoroacetic acid (2 mL) was added to the reaction mass and stirred for 19 hours with continuous air bubbling at the same temperature to afford the title product.
HPLC Purity: 59.1 1 %
Example 10: Preparation of Crude Linaclotide using solid supported TEMPO
To a mixture of water (100 mL) and silica bound TEMPO (0.01 g), linear chain of peptide of formula (I) (0.1 g) and sodium hypochlorite solution (1 mL) were added and the reaction mass was stirred 18 hours at 25 °C. Another lot of sodium hypochlorite solution (0.5 mL) was added to the reaction mass and stirred for further 7 hours at the same temperature to afford title product.
HPLC Purity: 42.70%………………see more in patent
|Systematic (IUPAC) name|
|Licence data||US FDA:|
|Molar mass||1526.74 g/mol|
///////WO 2016012938, DR. REDDY’S LABORATORIES LIMITED , Telangana, INDIA , Hyderabad, LINACLOTIDE, new patent
Process Development for Low Cost Manufacturing on 23-24 nov 2015 , Hyderabad, INDIA
- 23.11.2015 – 24.11.2015
- Hotel Green Park – Hyderabad, India
- View Brochure
- or click
Chemical process research and development is recognised as a key function during the commercialisation of a new product particularly in the generic and contract manufacturing arms of the chemical, agrochemical and pharmaceutical industries.
The synthesis and individual processes must be economic, safe and must generate product that meets the necessary quality requirements.
This 2-day course presented by highly experienced process chemists will concentrate on the development and optimisation of efficient processes to target molecules with an emphasis on raw material cost, solvent choice, yield improvement, process efficiency and work up, and waste minimisation.
Process robustness testing and reaction optimisation via stastical methods will also be covered.
A discussion of patent issues and areas where engineering and technology can help reduce operating costs.
The use of engineering and technology solutions to reduce costs will be discussed and throughout the course the emphasis will be on minimising costs and maximising returns.
Route selection, raw material choice
• Choosing the best route
• Using the cheapest raw materials and reagents, back integration of raw material supply
• Reducing the number of steps vs. reagent choice / yield and cost
• Solvent cost, recyclability
• Solvent reactivity and solvent swapping
• Solvent choice for reaction and work up
• Reaction understanding
• Improving conversion, selectivity
• Reaction quench
• Work up
• Product isolation (crystallisation, filtration and drying)
Statistical methods of optimisation
• Design of experiments
• Factorial and fractional factorial design
• Response surface analysis
• Robustness testing
Regulatory and Quality issues
• Impurity control and tracking
• Process validation and QbD
• Vessel cleaning
• Patents basics
• Patent definition
• Where patents are in force
• How to work around patents
Use of technology and engineering
• Flow chemistry
• SMB chromatography
• Separation technologies
At the end of the course participants will have gained:
• A logical investigative approach to chemical development and optimisation
• An insight into the factors involved in development and scaleup
• A preliminary knowledge of statistical methods of optimisation
• Improved ability to decide which parts of the chemical process to examine in detail.
• Ideas for efficient resource allocation
• Improved troubleshooting and problem solving ability
• A basic outline of the patent system
• An appreciation of how to assess the main cost contributors in a process