Merck + Co., Inc.

Audrey Molina

Ralph P Volante

Ioannis N Houpis

Joseph E Lynch

Peter G Houghton

Nobuyoshi Yasuda

Woo-Baeg Choi

Paul J Reider

Alan W Douglas

Ilias K Dorziotis

Hywyn R Churchill

Joannis Houpis

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

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.

Method of preparing phosphodiesterase IV inhibitors

The present invention is directed to a novel 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.

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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Ocean, NJ, United States of America

Audrey Molina