Technical scale synthesis of a new and highly potent thrombin inhibitor

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

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

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被引用次数: 12

摘要

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 ...