Sandoz Gmbh

Johnson Matthey Inc.

Massachusetts Institute of Technology

Novartis Ag

Johnson Matthey Public Limited Company

Oljan Repic

Prasad Koteswara Kapa

Thomas J Blacklock

David Xu

George T Lee

Goetz E Hardtmann

Timothy F Jamison

Susi Vogt

Urs Giger

Megan Alene Foley

The present invention provides a novel process for opening a lactone and/or a lactam ring. More particularly, the present invention provides a process that employs a novel catalyst in the opening of a lactone ring and/or a lactam ring. Additionally, the present invention also provides a novel deprotection process of any protecting group present in either the lactone ring-containing and/or lactam ring-containing compound and/or in the ring-opened product thereof.

Ring opening of lactones and lactams

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.

A process for synthesizing compounds of the formula ##STR1## utilizing, as intermediates, oxalyl chloride or bromide and compounds of the formulae R.sub.1 R.sub.2 N--CHO and CH.sub.2 .dbd.CH--O--R.sub.10 are processes for synthesizing compounds of the formula ##STR2## utilizing, as intermediates, compounds of Formula I wherein R.sub.1 is phenyl or substituted phenyl or intermediates in the synthesis of the compounds of formula I which intermediates have the formula ##STR3## wherein R.sub.1 is C.sub.1-3 alkyl, phenyl or phenyl substituted by 1 to 3 substituents each of which is independently C.sub.1-3 alkyl, C.sub.1-3 alkoxy, fluoro, chloro, bromo or nitro (maximum of two nitro groups),

Processes for the synthesis of 3-(substituted

Process for the synthesis of compounds of the formula ##STR1## comprising the steps of (i) reacting a compound of the formula ##STR2## with oxalyl chloride or oxalyl bromide to form the corresponding compound of the formula ##STR3## (ii) reacting said compound of the formula ##STR4## with a compound of the formula ##STR5## to form the corresponding compound of the formula ##STR6## (iii) hydrolyzing said compound of the formula ##STR7## to obtain the corresponding compound of the formula ##STR8## the use of the compounds of the formula ##STR9## for the synthesis of the compounds of the formula ##STR10## and the use of the intermediates of Formula VII for the direct synthesis of the compounds of Formula II, wherein

Processes for the synthesis of 3-disubstituted aminoacroleins

The invention provides a method of converting ethylenically unsaturated units of an olefinic substrate to corresponding cyclopropanyl units, comprising treating the olefinic substrate, in an ether medium, with zinc and diiodomethane and a catalytic amount of a metallo-hydride reducing agent. Preferred substrates are olefinic fatty acids or their functional derivatives, e.g. oleic acid esters.

Cyclopropanation of olefins

Conversion of 3-acyloxy-benzodiazepin-2-ones into corresponding 3-hydroxy benzodiazepin-2-ones is carried out efficiently with potassium hydroxide or potassium alkoxide as catalyst in lower alkanol solvent at a pH of 11-11.5. The final products, which include temazepam, are useful as sleep inducers.

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Randolph, NJ, United States of America

Oljan Repic