Warner-lambert Company

Senomyx, Inc.

James R Zeller

Ronald E Seamans

Rex A Jennings

Don R Johnson

Kevin Robert Wirtz

James N Wemple

Rhondi Shigemura

Boriruck Kitisin

Jennifer Ward

Carolyn Podgurski

Thitiwan Lebien

Maria Suparno

Mark J Suto

Victor Fedij

John Michael Domagala

Randall L De Jong

The present invention provides compositions comprising sucralose and 4-amino-5,6-dimethylthieno[2,3-d]pyrimidine-2(1H)-one or salts, solvates, and/or esters thereof and methods of making the compositions by spray drying. The present invention also provides ingestible compositions comprising compositions of the present invention and methods of making such foods. The present invention also includes a process of preparing 2-amino-thiophene derivatives, which are key intermediates for preparing 4-amino-5,6-dimethylthieno[2,3-d]pyrimidine-2(1H)-one.

Sweetner compositions and methods of making them

Sweetener compositions and methods of making them

The present invention provides compositions comprising sucralose and 4-amino-5,6-dimethylthieno [2,3-d]pyrimidine-2(1H)-one or salts, solvates, and/or esters thereof and methods of making the compositions by spray drying. The present invention also provides ingestible compositions comprising compositions of the present invention and methods of making such foods. The present invention also includes a process of preparing 2-amino-thiophene derivatives, which are key intermediates for preparing 4-amino-5,6-dimethylthieno[2,3-d]pyrimidine-2(1H)-one.

Novel cyanocycloalkylacetic acids and esters as well as salts thereof and in particular 1-cyanocyclohexaneacetic acid and ethyl 1-cyanocyclohexaneacetate are described which are useful as intermediates in a process for the preparation of cyclic amino acids.

Cyanocycloalkylacetic acid and ester intermediates for preparing cyclic

Chiral 3-cyanopyrrolidines of the following formula are disclosed, wherein R' is as defined herein. The compounds are useful as intermediates for naphthyridine and quinoline antibiotics. ##STR1##

Chiral 3-cyano-1-substituted-pyrrolidines

An improved process for the preparation of 2-amino-3,5-dihydro-7-substituted-4H-pyrrolo[3,2-d]pyrimidin-4-ones is described wherein 2,6-diamino-3,5-dihydro-7-substituted-4H-pyrrolo[3,2-d]pyrimidin-4-one is converted to a diazonium salt which is subsequently catalytically hydrogenated to the desired compound, as well as valuable intermediates used in the process.

Process for the synthesis of

An improved process for the preparation of cyclic amino acids by a novel synthesis is described where a dinitrile derivative is converted in two steps to the desired products, as well as valuable intermediates used in the process.

Process for cyclic amino acid anticonvulsant compounds

The process for the preparation of chiral 3-(1-amino-1,1-bisalkylmethyl)-1-substituted-pyrrolidines used as key intermediates for the preparation of naphthyridine and quinolone antibacterial agents which comprises reacting readily available chiral 1-substituted-3-pyrrolidinols to their corresponding chiral sulfonate esters; converting the sulfonate esters to chiral 1-substituted-3-cyanopyrrolidines having an inverse configuration, and then dialkylating the chiral cyanopyrrolidines with alkyl lithium in the presence of a Lewis acid without racemization at the asymmetric carbon atom is described.

Process for chiral

An improved process for the preparation of 7-substituted amino-1-alkyl- or cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids is described where tetrafluorobenzoyl chloride is converted in three operations via 1-alkyl or 1-cycloalkyl-1,4-dihydro-6,7,8-trifluoro-4-oxoquinoline-3-carbonitrile which in a separate step or in situ is displaced and hydrolyzed to the desired product.

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Holland, MI, United States of America

James R Zeller