Ioannis Houpis - Plainfield NJ Ralph P. Volante - Cranbury NJ Fengrui Lang - Piscataway NJ Ilias Dorziotis - Bridgewater NJ David Tschaen - Holmdel NJ Shinji Kato - Nagoya NJ Toshiaki Mase - Okazaki NJ
Assignee:
Merck Co., Inc. - Rahway NJ Banyu Pharmaceutical Co., Ltd, - Tokyo
International Classification:
C07D31734
US Classification:
549267
Abstract:
Michael addition conducted in the presence of a zinc-amine complex and additional amounts of the amine component results in product with high diastereomeric excess.
Convergent Process For The Preparation Of A Growth Hormone Secretagogue
Ilias Dorziotis - Bridgewater NJ Ioannis Houpis - Plainfield NJ Audrey Molina - Clark NJ Ralph Volante - Cranbury NJ
Assignee:
Merck & Co., Inc. - Rahway NJ
International Classification:
C07D40100
US Classification:
546 18
Abstract:
The present invention is directed to a novel convergent process for the preparation of the compound N-[1(R)-[(1,2-dihydro-1-methanesulfonyl-spiro[3H-indole-3,4'-piperdin]-1'- yl)carbonyl]-2-(phenylmethyl-oxy)ethyl]-2-amino-2-methyl-propanamide, and salts thereof, which has the structure: ##STR1## and which has the ability to stimulate the release of natural or endogenous growth hormone. This compound may be used to treat conditions which require the stimulation of growth hormone production or secretion such as in humans with a deficiency of natural growth hormone or in animals used for food or wool production where the stimulation of growth hormone will result in a larger, more productive animal.
Process For Making Phenyl Heterocycles Useful As Cox-2 Inhibitors
Ilias K. Dorziotis - Bridgewater NJ Ioannis N. Houpis - Plainfield NJ Jaemoon Lee - Edison NJ Ralph P. Volante - Cranbury NJ
Assignee:
Merck & Co., Inc. - Rahway NJ
International Classification:
C07D21330 C07D213127
US Classification:
546339
Abstract:
This invention is concerned with a novel process for the preparation of a compound of structural formula I ##STR1## wherein R. sup. 1 and R. sup. 2 independently are aryl, C. sub. 2-15 alkenyl or C. sub. 1-15 alkyl, either unsubstituted or substituted with one or three substituents, which can be the same or different, selected from the group consisting of R. sup. a, wherein R. sup. a belongs to a group consisting of C. sub. 1-6 alkyl, aryl, halo, --N(R. sup. 3). sub. 2, --NO. sub. 2, --CN, --OR. sup. 3, --C. sub. 3-6 cycloalkoxy, --CO(R. sup. 3), --COOR. sup. 3, SO. sub. 2 R. sup. 3 and --SR. sup. 3 ; wherein R3 is selected from the group consisting of hydrogen, C. sub. 1-6 alkyl, C. sub. 2-6 alkenyl and aryl, said alkyl, alkenyl or aryl optionally substituted with 1 to 3 groups of R. sup. a, which is an important antiasthmatic agent.
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