New Drug Approvals

Home » radio labelled » Fluorodopa F 18, フルオロドパ (18F), флуородопа (18F) , فلورودوبا (18F) , 氟[18F]多巴 ,

Fluorodopa F 18, フルオロドパ (18F), флуородопа (18F) , فلورودوبا (18F) , 氟[18F]多巴 ,

DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO .....FOR BLOG HOME CLICK HERE

ORGANIC SPECTROSCOPY

Read all about Organic Spectroscopy on ORGANIC SPECTROSCOPY INTERNATIONAL 

Categories

Blog Stats

  • 4,186,996 hits

Enter your email address to follow this blog and receive notifications of new posts by email.

Join 2,792 other subscribers

add to any

Share

92812-82-3.png

ChemSpider 2D Image | Fluorodopa F 18 | C9H1018FNO4

Fluorodopa F 18

2019/10/10, fda 2019,

Formula
C9H10FNO4
Cas
92812-82-3
Mol weight
215.1784

Diagnostic aid (brain imaging), Radioactive agent, for use in positron emission tomography (PET)

CAS 92812-82-3

フルオロドパ (18F)

L-6-(18F)Fluoro-DOPA
L-Tyrosine, 2-fluoro-18F-5-hydroxy- [ACD/Index Name]
флуородопа (18F) [Russian] [INN]
فلورودوبا (18F) [Arabic] [INN]
氟[18F]多巴 [Chinese] [INN]
((18)F)FDOPA
2-(fluoro-(18)F)-5-hydroxy-L-tyrosine
2-(Fluoro-18F)-5-hydroxy-L-tyrosine
2-(Fluoro-18F)-L-DOPA
2C598205QX
6-((18)F)fluoro-L-DOPA
6-(18F)Fluoro-L-DOPA
6692
(18F)FDOPA
2-((18)F)fluoro-5-hydroxy-L-tyrosine

Fluorodopa, also known as FDOPA, is a fluorinated form of L-DOPA primarily synthesized as its fluorine-18isotopologue for use as a radiotracer in positron emission tomography (PET).[1] Fluorodopa PET scanning is a valid method for assessing the functional state of the nigrostriatal dopaminergic pathway. It is particularly useful for studies requiring repeated measures such as examinations of the course of a disease and the effect of treatment

In October 2019, Fluorodopa was approved in the United States for the visual detection of certain nerve cells in adult patients with suspected Parkinsonian Syndromes (PS).[2][3]

The U.S. Food and Drug Administration (FDA) approved Fluorodopa F 18 based on evidence from one clinical trial of 56 patients with suspected PS.[2] The trial was conducted at one clinical site in the United States.[2]

PAPER

 Organic & Biomolecular Chemistry (2019), 17(38), 8701-8705

A one-pot two-step synthesis of 6-[18F]fluoro-L-DOPA ([18F]FDOPA) has been developed involving Cu-mediated radiofluorination of a pinacol boronate ester precursor. The method is fully automated, provides [18F]FDOPA in good activity yield (104 ± 16 mCi, 6 ± 1%), excellent radiochemical purity (>99%) and high molar activity (3799 ± 2087 Ci mmol−1), n = 3, and has been validated to produce the radiotracer for human use.

Graphical abstract: One-pot synthesis of high molar activity 6-[18F]fluoro-l-DOPA by Cu-mediated fluorination of a BPin precursor
Radiosynthesis of [ 18F]6F-l-DOPA The synthesis of [ 18F]6F-l-DOPA was fully-automated using a General Electric (GE) TRACERLab FXFN synthesis module (Figure S1) loaded as follows: V1: 500 µL 15mg/mL TBAOTf + 0.2 mg/mL Cs2CO3 in water; V2: 1000 µL acetonitrile; V3: 4 µmol Bpin precursor, 20 µmol Cu2+ , 500 µmol pyridine in 1 mL DMF; V4: 0.2 mL 0.25 M ascorbic acid + 0.6 mL 12.1 N HCl; V6: 3 mL acetonitrile; V7: 10 mL 0.9% saline, USP; V8: 2 mL ethanol, USP; Dilution flask: 100 mL acetonitrile ; F18 separation port: QMA cartridge ; C18 port: Strata cartridge.

PATENT

KR 2019061368

The present invention relates to an L-dopa precursor compd., a method for producing the same, and a method for producing 18F-labeled L-dopa using the same.  The method of prepg. 18F-labeled L-dopa I using the L-dopa precursor II [A = halogen-(un)substituted alkyl; W, X, Y = independently protecting group] can improve the labeling efficiency of 18F.  After the labeling reaction, sepn. and purifn. steps of the product can be carried out continuously and it can be performed with on-column labeling (a method of labeling through the column).  The final product I, 18 F-labeled L-dopa, can be obtained at a high yield relative to conventional methods.  Further, it has an advantage that it is easy to apply various methods such as bead labeling.

PAPER

Science (Washington, DC, United States) (2019), 364(6446), 1170-1174.

PAPER

European Journal of Organic Chemistry (2018), 2018(48), 7058-7065.

PATENT

WO 2018115353

CN 107311877

References

  1. ^ Deng WP, Wong KA, Kirk KL (June 2002). “Convenient syntheses of 2-, 5- and 6-fluoro- and 2,6-difluoro-L-DOPA”. Tetrahedron: Asymmetry13 (11): 1135–1140. doi:10.1016/S0957-4166(02)00321-X.
  2. Jump up to:a b c “Drug Trials Snapshots: Fluorodopa F 18”U.S. Food and Drug Administration (FDA). 27 November 2019. Archived from the original on 27 November 2019. Retrieved 27 November 2019. This article incorporates text from this source, which is in the public domain.
  3. ^ “Drug Approval Package: Fluorodopa F18”U.S. Food and Drug Administration (FDA). 20 November 2019. Archived from the original on 27 November 2019. Retrieved 26 November 2019. This article incorporates text from this source, which is in the public domain.
Fluorodopa
Fluorodopa.png
Clinical data
Other names 6-fluoro-L-DOPA, FDOPA
License data
Legal status
Legal status
Identifiers
CAS Number
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
Formula C9H10FNO4
Molar mass 215.18 g/mol g·mol−1
3D model (JSmol)

//////////////////Fluorodopa F 18, フルオロドパ (18F), FDA 2019, флуородопа (18F) فلورودوبا (18F) 氟[18F]多巴 , radio labelled

N[C@@H](CC1=CC(O)=C(O)C=C1[18F])C(O)=O


Leave a Reply

Fill in your details below or click an icon to log in:

WordPress.com Logo

You are commenting using your WordPress.com account. Log Out /  Change )

Twitter picture

You are commenting using your Twitter account. Log Out /  Change )

Facebook photo

You are commenting using your Facebook account. Log Out /  Change )

Connecting to %s

This site uses Akismet to reduce spam. Learn how your comment data is processed.

DR ANTHONY CRASTO

Follow New Drug Approvals on WordPress.com

Enter your email address to follow this blog and receive notifications of new posts by email.

Join 2,792 other subscribers
DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO Ph.D

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 amcrasto@gmail.com, 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......https://newdrugapprovals.wordpress.com/ , 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

Personal Links

View Full Profile →

TWITTER

  • RT @guptaakhilesh63: Look forward to deliberations at Inception meeting of #RIIG at Kolkata on 8th Feb 2023. @srivaric Secy @IndiaDST will… 2 hours ago
  • RT @dst_neelima: Had an interactive session with the UK delegation from British Geological Survey for leveraging Indo -UK collaborations on… 3 hours ago
  • RT @IndiaDST: The 2nd SCO Young Scientists Conclave #SCO_YSC is being hosted @jncasr , an autonomous institute of @IndiaDST , at its campus… 1 day ago
  • RT @SciUp: Our Understanding Polymorphism online course is only a week away! This five-session course aims to give chemists and engineers a… 1 day ago
  • RT @SciUp: Join us in Boston, US in May to get up-to-date intel on #flowchemistry. Our '5th Flow Chemistry & Continuous Processing' Confer… 1 day ago
  • RT @SciUp: Join us online for our 'Work Up and Product Isolation' short course on 23-24 February & you will lean how to design simple and p… 1 day ago
  • RT @thomasraji: Happy Birthday Mummyji !! Thanks for all your support and your invaluable life lessons.😍😍🎂💐💐🤩 You're not getting older...… 1 day ago
  • RT @GuwahatiNiper: 74वें गणतंत्र दिवस कार्यक्रम की झलकियां। Glimpses of the 74th Republic Day programme. @Pharmadept @rajneeshtingal @bhagw2 days ago
  • RT @dst_neelima: DST supported NCoE on CCU at IITB was the knowledge partner in the parallel event organised by ETWG G20 on CCUS on 5 th Fe… 2 days ago
  • RT @dst_neelima: Glad to represent DST India In an International Conference on CCUS organised as a parallel event to Energy Transition Work… 2 days ago
  • Glimpse of 2nd National One Day Symposium on “Drug Discovery Research in India: Current State and Future Prospects… twitter.com/i/web/status/1… 3 days ago
  • RT @africureonline: World Cancer Day is observed annually on February 4th to raise awareness about the impact of cancer on individuals and… 3 days ago
  • RT @CSIRCIMAP: Activity 13: Dr N Kalaiselvi, DG CSIR & Secretary, DSIR under #CSIR_OneWeekOneLab inaugurated the ‘High Throughput Instrumen… 4 days ago
  • Career counseling to pharma students, At Govindrao Nikam College Of Pharmacy Sawarde,Tal - Chiplun, Ratnagiri, Mh 4… twitter.com/i/web/status/1… 4 days ago
  • RT @bluetech_media: We are proud to welcome Dr.@Anthony Melvin Crasto Advisor Africure Pharma, Global A WDT API INT RnD, Ex Glenmark LS, Wo… 4 days ago

bloglovin

Follow my blog with Bloglovin The title of your home page You could put your verification ID in a comment Or, in its own meta tag Or, as one of your keywords Your content is here. The verification ID will NOT be detected if you put it here.
%d bloggers like this: