A Highly Convergent Synthesis of a Fibrinogen Receptor Antagonist

…, RJ Cvetovich, FR Tsay, JS Amato, B Pipik…

Index: Hartner, Frederick W.; Cvetovich, Raymond J.; Tsay, Fuh-Rong; Amato, Joseph S.; Pipik, Brenda; Grabowski, Edward J. J.; Reider, Paul J. Journal of Organic Chemistry, 1999 , vol. 64, # 21 p. 7751 - 7755

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Citation Number: 6

Abstract

A practical multikilogram synthesis of 2 (S)-[(p-toluenesulfonyl) amino]-3-[[[5, 6, 7, 8- tetrahydro-4-oxo-5-[2-(piperidin-4-yl) ethyl]-4 H-pyrazolo [1, 5-a][1, 4] diazepin-2-yl] carbonyl] amino] propionic acid pentahydrate (1), an oral fibrinogen receptor antagonist, is described. The nine-step convergent process, which afforded 1 in 37% overall yield, included pyrazole 5a and N-tosylaminoalanine 16 as key fragments. Pyrazole 5a was ...

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