PREPARATION OF 2S,3S-N-ISOBUTYL-N-(2- HYDROXY-3-AMINO-4-PHENYLBUTYL)-P- NITROBENZENESULFONYLAMIDE HYDROCHLORIDE AND OTHER DERIVATIVES OF 2-HYDROXY-l,3- DIAMINES

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چکیده

The present invention provides a new process for the preparation of 2S,3S-N-isobutyl-N-(2-hydroxy-3-amino-4phenylbutyl)-p-nitrobenzenesulfonylamide hydrochloride, wherein this compound is prepared directly from the chloromethylalcohol. Importantly, the process of the present invention results in higher yields of 2S,3S-N-isobutyl-N-(2hydroxy -3 -amino -4-phenylbu tyl) -pnitrobenzenesulfonylamide hydrochloride without sacrificing its purity. The processes of the present invention can be used to prepare not only the 2S,3S-derivative, but also the 2R,3S-, 2S,2Rand the 2R,3R-derivatives. (57) 27 Claims, 1 Drawing Sheet Related U.S. Application Data US 2003/0181723 A1 Sep. 25, 2003 Appl. No.: 10/382,185

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PREPARATION OF 2S,3S-N-ISOBUTYL-N-(2- HYDROXY-3-AMINO-4-PHENYLBUTYL) -P- NITROBENZENESULFONYLAMIDE HYDROCHLORIDE AND OTHER DERIVATIVES OF 2-HYDROXY-l,3- DIAMINES

Inventors: Aslam A. Malik, Cameron Park, CA (US); Hasan Palandoken, Woodland, CA (US); Joy A. Stringer, Carmichael, CA (US); Roland P. Carlson, Folsom, CA (US); John Leach, Gold River, CA (US); Thomas G. Archibald, Fair Oaks, CA (US); Robert G. Miotke, Gold River, CA (US) PREPARATION OF 2S,3S-N-ISOBUTYL-N-(2HYDROXY-3-AMINO-4-PHENYLBUTYL) -PNITROBENZENESULFONYLAMIDE HYDROCHLORIDE AND OTHER DERIV...

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تاریخ انتشار 2011