Merck + Co., Inc.

Other

Ioannis N Houpis

Ralph P Volante

Audrey Molina

Joseph E Lynch

Ilias K Dorziotis

Nobuyoshi Yasuda

Woo-Baeg Choi

David M Tschaen

Paul J Reider

Shinji Kato

Toshiaki Mase

Alan W Douglas

Kan K Eng

Jaemoon Lee

Hywyn R Churchill

Peter G Houghton

Fengrui Lang

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.

Diastereoselective preparation of Michael adducts

The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1##

Process for making phenyl heterocycles useful as COX-2 inhibitors

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.

Convergent process for the preparation of a growth hormone secretagogue

Process for the preparation of a growth hormone secretagogue

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.

Method of preparing phosphodiesterase IV inhibitors

A process for the preparation of a compound of structural formula I ##STR1## wherein R.sup.1 is alkyl, alkenyl, phenyl or substituted phenyl, which comprises the addition of R.sup.1 to an intermediate 2: ##STR2## by treatment of 2 with (R.sup.1).sub.3 M followed by reductive removal of the sulfinyl group.

A process is disclosed for rapid synthesis of substituted furanyl pyridines.

Method of synthesizing furo[2,3-b]pyridine carboxylic acid esters

4-Chloro-2-cyclopropylcarbonylaniline is prepared by condensation of 4-chloroaniline with 4-chlorobutyronitrile to form a 2-(4-chlorobutyryl)-4-chloroaniline, followed by ring closure of the 4-chlorobutyryl group to a cyclopropylcarbonyl moiety.

Process for the preparation of 4-chloro-2-cyclopropylcarbonylaniline

A process for preparing optically pure decahydroisoquinolines in good yields which avoids difficult purification procedures is described.

Process for optically pure decahydroisoqiunolines

An efficient process for the preparation of styrylbenzoxazoles and derivatives thereof comprises reacting a methylbenzoxazole with an aromatic aldehyde in the presence of strong base at low temperature, followed by warming. The condensation products are inhibitors of H.sup.+ K.sup.+ -ATPase, and are also useful as penultimate compounds in the preparation of inhibitors of HIV reverse transcriptase.

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Edison, NJ, United States of America

Ioannis N Houpis