Ramesh N. Patel - Bridgewater NJ Amit Banerjee - St. Louis MO Venkata B. Nanduri - East Brunswick NJ Steven L. Goldberg - Basking Ridge NJ Robert M. Johnston - Whitehouse Station NJ Thomas P. Tully - Middlesex NJ Laszlo J. Szarka - East Brunswick NJ Shankar Swaminathan - North Brunswick NJ John J. Venit - North Brunswick NJ Jerome L. Moniot - Chester NJ William J. Winter - New Brunswick NJ Neal G. Anderson - Stockton NJ David A. Lust - Roosevelt NJ Gerard Crispino - Princeton NJ Sushil K. Srivastava - Dayton NJ
Assignee:
Bristol-Myers Squibb Co. - Princeton NJ
International Classification:
C07C 3200
US Classification:
562432, 562433, 562426, 562485, 562400
Abstract:
The present invention concerns an enzymatic oxidative deamination process of a dipeptide monomer to prepare an intermediate useful to prepare compounds having endopeptidase and angiotensin converting enzyme inhibition activity.
Neal G. Anderson - Somerset NJ David A. Lust - Roosevelt NJ Barbara J. Bennett - North Brunswick NJ Alan F. Feldman - Philadelphia PA Robert E. Polomski - Franklin Park NJ
Assignee:
E. R. Squibb & Sons, Inc. - Princeton NJ
International Classification:
C07D20708
US Classification:
548533
Abstract:
A process is disclosed for direct isolation of captopril from a substrate of the formula ##STR1## wherein R is lower alkyl or lower alkoxy. In this process, the substrate is first treated with an aqueous alkali metal hydroxide capable of forming a water-soluble salt of the substrate, wherein the alkali metal hydroxide has a concentration of 4M or greater. The substrate is then neutralized, preferably with a mineral acid. By this process, captopril may be directly crystallized from an aqueous solution, avoiding the prior art use of organic solvents and zinc treatment to reduce levels of sulfide and disulfide impurities, respectively. In an alternative embodiment, neutralization is carried out by use of a hydrogen-supplying ion exchange resin.
Process For Stereochemically Inverting A Hydroxy Function Of An Ester By A Modified Mitsunobu Reaction Process
Neal G. Anderson - Somerset NJ Christopher M. Cimarusti - Somerset NJ David A. Lust - Roosevelt NJ
Assignee:
E. R. Squibb & Sons, Inc. - Princeton NJ
International Classification:
C07D20700
US Classification:
548533
Abstract:
A process is provided for inverting a hydroxy function of a L-trans-hydroxy proline derivative to the corresponding L-cis-hydroxy proline sulfonate by a Modified Mitsunobu reaction process.