- AMIDE COMPOUNDS
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The present invention provides compounds represented by the formula (Ia) the formula (Ib) the formula (Ic) and the formula (Id) wherein each symbol is as defined in the specification. According to the present invention, these compounds have a DGAT inhibit
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Page/Page column 255
(2008/06/13)
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- Technical scale synthesis of a new and highly potent thrombin inhibitor
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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 intermediate dehydroproline 22 and the transformation of nitriles into amidines. The thrombin inhibitor 1 was isolated by special techniques (nanofiltration and spray drying). Almost all salts of 1 are amorphous, however, a crystalline complex was obtained with 1,2-benzisothiazol-3(2H)-one 1,1-dioxide (Saccharin).
- Bernard, Harald,Buelow, Gerd,Lange, Udo E. W.,Mack, Helmut,Pfeiffer, Thomas,Schaefer, Bernd,Seitz, Werner,Zierke, Thomas
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p. 2367 - 2375
(2007/10/03)
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