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Sphaelactone dimethylamine fumarate



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Sphaelactone dimethylamine fumarate

Accenda Tech Co Ltd; Nankai University

Acute leukemia

Protein farnesyltransferase inhibitor; Ras GTPase inhibitor

Accendatech天津尚德药缘科技有限公司,Nankai University南开大学

 crystalline lactone dimethylamine fumaric and method of the present invention belongs to the field of pharmaceutical technology, in particular, relates to a lactone dimethylamine smile crystalline fumarate ship their preparation.  Patent CN 101978959 A discloses a lactone and derivatives thereof, pharmaceutical compositions for use in the treatment of cancer, including the formula (π) compounds, lactone dimethylamine. Activity test results show that the compounds of formula (Π) of the test cell comprising: HepG-2, Ec9706, SGC790K SW1116, A498, ASPC-1, H -29, HeLa, GL15, B16F1, T24, SKOV3, SW579, PC -3, are showing strong inhibitory activity; rather stab at 50 μ Μ normal cells, the filaments exhibit significant killing effect.

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WO 2011/131103 A1 discloses a formula including the inner (I) compound smile lactone derivative or a salt thereof a pharmaceutical composition, preparation and use for the preparation of anticancer drugs. But no problem about the compound of formula polymorph (I), have not been reported for formula (I) compounds of the crystalline areas. The present invention provides compounds of formula (I) dimethylamine smile lactone crystalline fumarate and its preparation method.

Figure imgf000003_0001

An object of the present invention to provide a compound of formula (I) a lactone compound smile dimethylamine i.e. crystalline fumarate polymorph A. Another object of the present invention to provide a method for preparing crystalline compound of formula (I). A lactone compound of dimethylamine fumaric polymorph A boat characteristics of formula (I):



Example 1:

11PH, 13 – two smiling Yue amino lactone (Compound II) (the structural formula of the formula (II)) Preparation of

Smile lactone (106 mg, 0.40 mmol), triethylamine (2.0mL), Yue alcohol (30 mL) was added lOO mL round bottom flask and heated at reflux for 3 hours, concentrated under reduced pressure, cross stone column chromatography (petroleum ether : ethyl acetate: triethylamine = 50: 50: 0.5) to give a white solid 107.4 mg, yield: 86%.

Formula: C 17 H 27 N0 3

Weight: 293

Appearance: white amorphous 4 minutes late

Spectral data:

¾ NMR (CDCl 3 , 400 MHz) delta 3.76 (t, J = 5.0 Hz, 1H), 2.96 (s, 1H), 2.49-2.67 (m, 3H), 2.28-2.34 (m, IH), 2.30-2.34 (m, 2H), 2.18 (s, 6H), 2.09 (br s, 2H), 1.96 (d, J = 11.2, IH), 1.67-1.73 (m, 2H), 1.60 (s, 3H) 1.22 (br s, 3H), 1.18 (br s, 2H); 13 C NMR (CDCl 3 , 100 MHz) delta 177.0, 131.8, 131.3, 84.0, 80.2, 58.3, 58.1, 50.9, 46.0, 44.6, 38.4, 35.3, 30.0, 27.2, 23.7, 22.8.



A new crystalline form of sphaelactone dimethylamine fumarate and its preparation are claimed. The parent compound is ACT-001 (DMAMCL) which Accenda Tech and Nankai University are investigating for potential oral treatment of acute leukemia. Preclinical studies were completed in October 2012, and an application for clinical trials was planned for 2013. Picks up from WO2013163936, which claims preparation of similar compounds.








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DR ANTHONY MELVIN CRASTO, Born in Mumbai in 1964 and graduated from Mumbai University, Completed his Ph.D from ICT, 1991,Matunga, Mumbai, India, in Organic Chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues, Currently he is working with AFRICURE PHARMA as ADVISOR, earlier assignment was with GLENMARK LIFE SCIENCES LTD, as CONSUlTANT, Retired from GLENMARK in Jan2022 Research Centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Total Industry exp 32 plus yrs, Prior to joining Glenmark, he has worked with major multinationals like Hoechst Marion Roussel, now Sanofi, Searle India Ltd, now RPG lifesciences, etc. He has worked with notable scientists like Dr K Nagarajan, Dr Ralph Stapel, Prof S Seshadri, etc, He did custom synthesis for major multinationals in his career like BASF, Novartis, Sanofi, etc., He has worked in Discovery, Natural products, Bulk drugs, Generics, Intermediates, Fine chemicals, Neutraceuticals, GMP, Scaleups, etc, he is now helping millions, has 9 million plus hits on Google on all Organic chemistry websites. His friends call him Open superstar worlddrugtracker. His New Drug Approvals, Green Chemistry International, All about drugs, Eurekamoments, Organic spectroscopy international, etc in organic chemistry are some most read blogs He has hands on experience in initiation and developing novel routes for drug molecules and implementation them on commercial scale over a 32 PLUS year tenure till date Feb 2023, Around 35 plus products in his career. He has good knowledge of IPM, GMP, Regulatory aspects, he has several International patents published worldwide . He has good proficiency in Technology transfer, Spectroscopy, Stereochemistry, Synthesis, Polymorphism etc., He suffered a paralytic stroke/ Acute Transverse mylitis in Dec 2007 and is 90 %Paralysed, He is bound to a wheelchair, this seems to have injected feul in him to help chemists all around the world, he is more active than before and is pushing boundaries, He has 100 million plus hits on Google, 2.5 lakh plus connections on all networking sites, 100 Lakh plus views on dozen plus blogs, 227 countries, 7 continents, He makes himself available to all, contact him on +91 9323115463, email, Twitter, @amcrasto , He lives and will die for his family, 90% paralysis cannot kill his soul., Notably he has 38 lakh plus views on New Drug Approvals Blog in 227 countries...... , He appreciates the help he gets from one and all, Friends, Family, Glenmark, Readers, Wellwishers, Doctors, Drug authorities, His Contacts, Physiotherapist, etc He has total of 32 International and Indian awards

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