PROCESS FOR PREPARING CHLORO ALCOHOL DERIVATIVES AND INTERMEDIATES

WIPO Patent Application WO/1999/054297

A1

A process for preparing compounds represented by general formula (X), comprising the steps of: saponifying a (2S,3R)-4-hydroxy-2,3-epoxybutanoic acid derivative; regioselectively opening the epoxy ring of the resultant derivative to obtain an open-ring derivative; protecting the amino group of the derivative; lactonizing the protected derivative; reducing the lactone derivative; protecting the 1- and 2-hydroxy groups of the reduced derivative; thioetherifying the protected derivative; removing the protective groups of the thioetherified derivative; and selectively chlorinating the primary hydroxyl group of the diol derivative; and novel intermediate compounds obtained in the course of the production of the compounds (X). The compounds (X) are useful as a key intermediate of the compound (XI) useful as an HIV protease inhibitor.

IKUNAKA MASAYA (JP)
MATSUMOTO JUN (JP)
FUJIMA YOSHITO (JP)
HIRAYAMA YOSHIHIKO (JP)

PCT/JP1998/001755

October 28, 1999

April 16, 1998

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NAGASE & CO LTD (JP)
IKUNAKA MASAYA (JP)
MATSUMOTO JUN (JP)
FUJIMA YOSHITO (JP)
HIRAYAMA YOSHIHIKO (JP)

C07C213/04; (IPC1-7): C07C323/44; C07C227/08; C07C229/22; C07C271/16; C07C271/22; C07C319/20; C07D303/48; C07D307/32; C07D317/28

WO1997011938A1	1997-04-03
WO1995009843A1	1995-04-13

JPS59106444A	1984-06-20
JPH09110809A	1997-04-28

PERCY S. MANCHAND et al., "A Novel Synthesis of the Monobactam Antibiotic Carumonam", J. ORG. CHEM., 1988, Vol. 53, No. 23, p. 5507-5512.

Yamamoto, Shusaku (15th floor 2-27, Shiromi 1-chome, Chuo-k, Osaka-shi Osaka, JP)

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