Merck + Co., Inc.

Michael A Wallace

Ralph P Volante

Ichiro Shinkai

David Askin

Richard L Monaghan

Prakash S Masurekar

Wesley L Shoop

An active avermectin analogue which can be produced by directed biosynthesis is described. The compound, named 26-R-Avermectin B.sub.1 a, is active in the Haemonchus egg to L3 assay and has the following structure: ##STR1##

Active avermectin analogue

An efficient process for stereoselective preparation of a medicinally significant hydroxyamide compound of structural formula: ##STR1## comprises the addition of metalated amide enolates to chiral .alpha.-amino metalated epoxides. The hydroxyamide reaction products are useful as inhibitors of the HIV protease or of renin, or as intermediates in the preparation of inhibitors of the HIV protease or renin.

Stereoselective production of hydroxyamide compounds from chiral

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Lebanon, NJ, United States of America

Michael A Wallace