Pharmacia Corporation

Monsanto Technology LLC

Serge G Wolfson

Patrick J Lennon

Gunnar J Hanson

Michael L Vazquez

Michael John Clare

Richard M Weier

Richard A Partis

Timothy J Hagen

Michael B Tollefson

Suzanne S Metz

Francis J Koszyk

Michael A Stealey

Bruce C Hamper

He Huang

Arija A Bergmanis

Xiangdong Xu

Subo Liao

Lifeng Geng

Shuyuan Liao

Joyce Zuowu Crich

Thomas Dale Owen

Stephen C Houdek

Scott B Mohler

Dominique Bonafoux

Donna M Iula

Theresa R Fletcher

Maria Nguyen

David S Oburn

Angela M Scates

James P Coleman

Samuel J Tremont

Jerry R Ebner

Eric A Haupfear

Joseph A Schaper

Philip H Brodsky

N-phosphonomethylamines are produced by reaction of an amine substrate with a halomethylphosphonic acid or salt thereof, a hydroxymethylphosphonic acid or salt thereof, or a dehydrated self-ester dimer, trimer or oligomer of hydroxymethylphosphonic acid. Among the products that may be prepared according to the process are N-phosphonomethylaminocarboxylic acids such as (e.g.) glyphosate, N-phosphonomethylaminoalkanols such as (e.g.) hydroxyethlaminomethylphosphonic acid, and N-acylaminomethylphosphonic acids such as (e.g.) N-carbamylaminomethylphosphonic acid. Certain reactions are conducted with a substantial excess of amine reactant in order to drive the conversion while avoiding excessive formation of bis(N-phosphonomethyl)amine by-products. Other reactions use a secondary amine substrate (such as iminodiacetic acid) and can be conducted at substantial equimolar ratios of halomethylaminomethylphosphonic acid or hydroxyaminomethylphosphonic acid to secondary amine reactant without significant formation of bis(phosphonomethyl)amine by-products. Further disclosed is a process for the preparation of hydroxymethylphosphonic acid self-ester dimers, trimers and oligomers by azeotropic dehydration.

Process for the preparation of N-phosphonomethylglycine and derivatives thereof

The present invention relates to substituted pyrazolyl derivatives, compositions comprising such, intermediates, methods of making substituted pyrazolyl derivatives, and methods for treating cancer, inflammation, and inflammation-associated disorders, such as arthritis.

Substituted pyrazolyl compounds for the treatment of inflammation

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Chesterfield, MO, United States of America

Serge G Wolfson