1. A new synthesis of the GPIIb/IIIa receptor antagonist SB-214857-A
- Author
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David O. Morgan, Richard J. Atkins, Andrew S. Wells, Stephen A. Smith, Gary F. Breen, Timothy Charles Walsgrove, Nigel Hussain, Ian P. Andrews, Jerome F. Hayes, John S. Carey, Neil F. Badham, Etridge Stephen K, Andrew C. Share, and Richard K. Bellingham
- Subjects
chemistry.chemical_classification ,biology ,medicine.drug_class ,Stereochemistry ,Organic Chemistry ,Alcohol ,Receptor antagonist ,Biochemistry ,Lotrafiban ,chemistry.chemical_compound ,GpIIb/IIIa ,Enzyme ,chemistry ,Drug Discovery ,medicine ,biology.protein ,Lipase - Abstract
A new synthesis of lotrafiban SB-214857-A is reported. The key steps are the preparation of racemic (4-methyl-3-oxo-2,3,4,5-tetrahydro-1H-benzo[e][1,4]diazepin-2-yl)-acetic acid methyl ester from 2-nitrobenzyl alcohol, a resolution using an immobilised lipase enzyme and a palladium-catalysed aminocarbonylation reaction.
- Published
- 2001
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