Novartis Ag

Johnson Matthey Inc.

Johnson Matthey Public Limited Company

David Xu

Prasad Koteswara Kapa

Thomas J Blacklock

Oljan Repic

Gottfried Sedelmeier

Murat Acemoglu

Olivier Loiseleur

Thomas Allmendinger

John Vincent Calienni

Wenming Liu

Jacques Cercus

A process for the production of a compound of Formula I, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable prodrug ester thereof, comprising cleaving a lactam of formula II 

Process for phenylacetic acid derivatives

The present invention relates to an improved process for preparing certain substituted caprolactam compounds which comprises acylating an aminocaprolactam compound with a lactone compound in the presence of a weak base and a polar, organic solvent, and hydrolyzing the resultant diamide compound in a mixture of solvents to obtain the desired caprolactam compound.

Process for preparing certain substituted caprolactams

An improved process for preparing 1,1'-�1,4-phenylenebis-(methylene)!-bis-1,4,8,11-tetraazacyclotetradecane comprising the selective functionalization of an acyclic tetraamine, and subsequent dimerization and hydrolyzation/tosylation to obtain a 1,4-phenylenebis-methylene bridged hexatosyl acyclic precursor in a first step, the cyclization of said precursor to obtain a hexatosyl cyclam dimer in a second step, and the detosylation of said cyclam dimer in a third step followed by basification to obtain the desired 1,1'-�1,4-phenylenebis-(methylene)!-bis-1,4,8,11-tetraazacyclotetradecane.

Process for preparing 1,1'- (1,4- phenylenebis (methlene)-Bis

Process for preparing

An improved process for preparing 1,1'-[1,4-phenylenebis-(methylene)]-bis-1,4,8,11-tetraazacyclotetradecane comprising the selective functionalization of an acyclic tetraamine, and subsequent dimerization and hydrolyzation/tosylation to obtain a 1,4-phenylenebis-methylene bridged hexatosyl acyclic precursor in a first step, the cyclization of said precursor to obtain a hexatosyl cyclam dimer in a second step, and the detosylation of said cyclam dimer in a third step followed by basification to obtain the desired 1,1'-[1,4-phenylenebis-(methylene)]-bis-1,4,8,11-tetraazacyclotetradecane.

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Whippany, NJ, United States of America

David Xu