Zeneca Limited

The Dupont Merck Pharmaceutical Company

Imperial Chemical Industries Limited

Bristol-myers Squibb Pharma Company

Dupont Pharmaceuticals Company

Bristol-myers Squibb Pharma Corporation

Gregory D Harris

Marc Jerome Chapdelaine

Joseph M Fortunak

Paul Francis Jackson

Robert E Waltermire

Luigi Anzalone

Lilian Alicia Radesca

Benjamin R P Stone

Ioannis I Valvis

William Aloysius Nugent

Stanley A Lee

Edward Koon Wat

Roberta L Dorow

Goss S Kauffman

Rodney L Parsons

Akin H Davulcu

This invention relates generally to the asymmetric synthesis of quinazolin-2-ones that are useful as inhibitors of HIV reverse transcriptase. The synthesis is accomplished through the chiral ligand mediated addition of cyclopropylacetylide.

Asymmetric synthesis of quinazolin-2-ones useful as HIV reverse transcriptase inhibitors

Preparation of asymmetric cyclic ureas through a monoacylated diamine intermediate

Benz�b!azepine compounds, pharmaceutical compositions containing them and methods for the treatment of neurological disorders utilizing them.

Therapeutic compositions

Benz[b]azepine compounds, pharmaceutical compositions containing them and methods for the treatment of neurological disorders utilizing them.

This invention provides improved synthetic processes for the preparation of hydroxy-protected cyclic urea compounds of Formula (IX), ##STR1## which are useful as intermediates for the preparation of cyclic urea human immunodeficiency virus (HIV) protease inhibitors, from N-protected aminoaldehydes. The processes of the present invention provide high yields, can be conducted on multikilogram scale, and eliminate the need for chromatographic purification of intermediates or final product.

Method for preparing cyclic ureas and their use for the synthesis of HIV

A method for the isolation and purification of an imidazole compound, useful as an angiotensin II receptor inhibitor compound or as a key intermediate therefor, from a mixture of it with its regioisomer in a solvent by treament of the mixture with a strong acid to effect selective precipitation of the desired regioisomeric imidazole salt.

Process for the isolation and purification of an imidazole stereoisomer

A method for isolating and purifying an ester functionalized imidazole compound, useful as an angiotensin (II) antagonist or as a key intermediate therefor, from a mixture of it with its regioisomer in a solvent, by treatment with an alkali metal hydroxide to achieve the regioselective hydrolysis of the undesired regioisomeric ester.

Process for the isolation and purification of ester functionalized

1-bolizazepin-2,5-diones

The invention concerns a novel process for the manufacture of various aryloxyaliphatic aldehydes and related arylthio analogues, which are useful as chemical intermediates. The process involves reacting a dihalogenohydroxyalkane of the formula: HO.C(R.sup.2).sub.2.CHX.sub.2 wherein R.sup.2 is alkyl and X is chloro or bromo with a phenol or thiophenol in the presence of base and is applicable to large scale use.

Process for manufacturing aryloxyaldehydes

The invention concerns a novel process for the stereospecific manufacture of novel hydroxymethyl lactols of the formula I by a one step reduction of a corresponding lactone carboxylic ester of the formula II (many of which esters are novel) using a reducing agent such as diisobutylaluminium hydride at about ambient temperature. The lactols of formula I are intermediates for the production of pharmacologically active 1,3-dioxane alkenoic acids useful in the treatment of certain cardiovascular and pulmonary medical conditions. Certain of the esters of formula II are novel and are also included in the invention.

Growing community of inventors

Wilmington, DE, United States of America

Gregory D Harris