Dupont Pharmaceuticals Company

E.i. Dupont De Nemours and Company

Other

The Dupont Merck Pharmaceutical Company

Michael Ernest Pierce

Lilian Alicia Radesca

John J Duncia

Paul E Aldrich

Anusuya Choudhury

Prabhakar Kondaji Jadhav

Dalian Zhao

Lushi Tan

Cheng Yi Chen

George C Emmett

Rodney Lawrence Parsons, Jr

Practical synthesis of benzoxazinones useful as HIV reverse transcriptase inhibitors

The present invention describes novel methods for the synthesis of benzoxazinone compounds which are useful as human immunodeficiency virus (HIV) reverse transcriptase inhibitors. The benzoxazinone of the formula: is particularly effective in the treatment of HIV.

Practical synthesis of benzoxazinones useful as HIV reverse

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

This invention relates to methods for preparing alkylating agents and use of the agents prepared. In particular, this invention relates to preparation methods for hydroxy halide and organooxy halide alkylating agents and their use for alkylating cyclic urea compounds.

Method for preparing alkylating agents for their use for alkylating

Method for preparing alkylating agents and their use for alkylating

Tetrazole intermediates useful to prepare antihypertensive compounds described in coassigned application U.S. Ser. No. 884,920, filed July 11, 1986, are described, these tetrazoles have the formula: ##STR1## wherein X.sup.1 and X.sup.2 are as described in the specification.

Tetrazole intermediates to antihypertensive compounds

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Wilmington, DE, United States of America

Michael Ernest Pierce