A Highly Convergent Synthesis of a Fibrinogen Receptor Antagonist

• Published in: Journal of organic chemistry Vol. 64; no. 21; pp. 7751 - 7755
• Main Authors: Hartner, Frederick W, Cvetovich, Raymond J, Tsay, Fuh-Rong, Amato, Joseph S, Pipik, Brenda, Grabowski, Edward J. J, Reider, Paul J
• Format: Journal Article
• Language: English
• Published: WASHINGTON American Chemical Society 15.10.1999; Amer Chemical Soc
• Subjects: Chemistry; Chemistry, Organic; Physical Sciences; Science & Technology; PEPTIDE MIMETICS; DESIGN; GLYCOPROTEIN IIB/IIIA INHIBITORS; 4-VINYLPYRIDINE

A practical multikilogram synthesis of 2(S)-[(p-toluenesulfonyl)amino]-3-[[[5,6,7,8-tetrahydro-4-oxo-5-[2-(piperidin-4-yl)ethyl]-4H-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...