Dupont Pharmaceuticals Company

Anusuya Choudhury

Michael Ernest Pierce

Lilian Alicia Radesca

Dalian Zhao

Lushi Tan

Cheng Yi Chen

Rodney Lawrence Parsons, Jr

The present invention relates generally to novel methods for the synthesis of cyclopropylacetylene which is an essential reagent in the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one; a useful human immunodeficiency virus (HIV) reverse transcriptase inhibitor.

Process for the preparation of cyclopropylacetylene

The present invention provides novel methods for the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1- benzoxazin-2-one of formula (VI-i) ##STR1## which is useful as a human immunodeficiency virus (HIV) reverse transcriptase inhibitor.

Asymmetric synthesis of benzoxazinones

Growing community of inventors

Landenberg, PA, United States of America

Anusuya Choudhury