Dow Agrosciences LLC

Merrell Pharmaceuticals, Inc.

Hoechst Marion Roussel

James R McConnell

James R McCarthy

Donald Paul Matthews

Douglas Bland

Jeffrey S Sabol

Richard E Donaldson

David E Podhorez

Robert Duquid

Ronald Ross, Jr

Gary A Roth

Kim Eric Arndt

Ronald B Leng

Todd William Toyzan

Robert Duguid

Douglas C Bland

Gary Alan Roth

2-Trifluoromethyl-5-(1-substituted)alkylpyridines of formula (I)    

Process for the preparation of 2-trifluoromethyl-5-(1-substituted)alkylpyridines

Alkylthio substituted aldehydes, ketones, esters and sulfones are prepared by reacting &#x3b1;,&#x3b2;-unsaturated carbonyl and sulfonyl compounds with a sodium or potassium thiolate in the presence of a alkane carboxylic acid and water.

Process for the addition of thiolates to &#x3b1;,&#x3b2;-unsaturated carbonyl or sulfonyl compounds

Cyano-substituted sulfilimines are produced efficiently and in high yield from the corresponding sulfides by reaction with cyanamide and hypochlorite.

Process for the preparation of certain substituted sulfilimines

Insecticidal sulfoximines are produced efficiently and in high yield by the oxidation of the corresponding sulfilimine with ruthenium tetraoxide or an alkali metal permanganate.

Process for the oxidation of certain substituted sulfilimines to insecticidal sulfoximines

The present invention is directed toward a novel process of preparing 2'-exocyclic vinylfluoride derivatives of cytidine analogues for use as ribonucleotide reductase inhibitors.

Process for the preparation of ribonucleotide reductase inhibitors

The present invention is directed toward a novel process of preparing 2'-exocyclic vinylfluoride derivatives of cytidine analogues for use as ribonucleotide reductase inhibitors. The novel process of the present invention utilizes a cytidine derivative as the required starting material and provides the ribonucleotide reductase inhibitor in a more efficient than the reaction sequence. The process is more efficient than the process disclosed by McCarthy et al. in European Patent Application Publication No. 0 372 268 published Jun. 13, 1990, in that it requires fewer chromatographies and results in an overall yield of greater than 25% for the five steps. The present invention further provides the ribonucleotide reductase inhibitor in a four step reaction sequence and results in an overall yield of greater than 35%.

The present invention is directed toward a novel process of preparing 2'-exocyclic vinylfluoride derivatives of cytidine analogues for use as ribonucleotide reductase inhibitors. The novel process of the present invention utilizes a cytidine derivative as the required starting material and provides the ribonucleotide reductase inhibitor in a more efficient five step reaction sequence. The present invention further provides the ribonucleotide reductase inhibitor in a four step reaction sequence and results in an overall yield of greater than 35%.

Growing community of inventors

Midland, MI, United States of America

James R McConnell