Process for preparing N-protected amino acid .alpha.-halomethyl

Details Process for preparing N-protected amino acid .alpha.-halomethyl Process for preparing N-protected amino acid .alpha.-halomethyl

1994-12-13

1996-01-02

Evans, Joseph E.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

560160, C07D30102, C07D30312, C07D30336

Patent

active

054810116

ABSTRACT:
The present invention relates to a novel method useful for the conversion of amino acids to halomethylketones, which are then converted to amino acid epoxides. Such epoxides are important intermediates for the synthesis of inhibitors of renin and HIV protease, which are particularly useful in the treatment and/or prevention of HIV infection (AIDS).

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Barluenga, et al, J. Chem. Soc., Chem. Commun., pp. 969-970 (1994).
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Wheeler, et al, J. Med. Chem., 22:657-661 (1979).
Kakeya, et al, Chem. Pharm. Bull., 32:692-698 (1984).
Harada, et al, Syn. Commun., 24:767-772 (1994).

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