Preparation of...

Organic compounds -- part of the class 532-570 series – Organic compounds – Amino nitrogen containing

Reexamination Certificate

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C560S029000, C564S483000

Reexamination Certificate

active

06852887

ABSTRACT:
The present invention provides a new process for the preparation of 2S,3S-N-isobutyl-N-(2-hydroxy-3-amino-4-phenylbutyl)-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-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamide 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,2R- and the 2R,3R-derivatives.

REFERENCES:
patent: 4760189 (1988-07-01), Mercier et al.
patent: 5585397 (1996-12-01), Tung et al.
patent: 5723490 (1998-03-01), Tung
patent: 5783701 (1998-07-01), Tung et al.
patent: 5874623 (1999-02-01), Adkins et al.
patent: WO 9405639 (1994-03-01), None
Parkes, et al.,J. Org. Chem.,59:3656 (1994).

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