Technical scale synthesis of a new and highly potent thrombin inhibitor

…, H Mack, T Pfeiffer, B Schaefer, W Seitz, T Zierke

Index: Bernard, Harald; Buelow, Gerd; Lange, Udo E. W.; Mack, Helmut; Pfeiffer, Thomas; Schaefer, Bernd; Seitz, Werner; Zierke, Thomas Synthesis, 2004 , # 14 p. 2367 - 2375

Full Text: HTML

Citation Number: 12

Abstract

Abstract In this account, we describe the development of an efficient and convergent process for the peptidomimetic thrombin inhibitor 1 on production plant scale. Starting from nicotinonitrile (13),(2S, 4R)-1-(tert-butoxycarbonyl)-4-hydroxy-2-pyrrolidinecarboxylic acid (5) and (2R)-2-amino-3-cyclohexylpropanoic acid (29) compound 1 was obtained in 16 chemical steps. New methods had been developed for the preparation of the key ...

Related Articles:

General and scalable amide bond formation with epimerization-prone substrates using T3P and pyridine

[Lange, Udo E.W.; Baucke, Dorit; Hornberger, Wilfried; Mack, Helmut; Seitz, Werner; Hoeffken, H. Wolfgang Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 10 p. 2648 - 2653]

Practical syntheses of 4-fluoroprolines

[Chorghade, Mukund S.; Mohapatra, Debendra K.; Sahoo, Gokarneswar; Gurjar, Mukund K.; Mandlecha, Manish V.; Bhoite, Nitin; Moghe, Santosh; Raines, Ronald T. Journal of Fluorine Chemistry, 2008 , vol. 129, # 9 p. 781 - 784]

More Articles...