Merck Sharp + Dohme Corp.

Nsab, Filial Af Neurosearch Sweden Ab, Sverige

Richard Desmond

Feng Xu

Jeonghan Park

Birgit Kosjek

Hongmei Li

Zhuqing Liu

Hallena Strotman

Alexei Kalinin

Johannah R Moncecchi

Paul N Devine

Guy R Humphrey

Richard John Varsolona

Yong-Li Zhong

Zhiguo Jake Song

Tao Wang

Ji Qi

Laura Marie Artino

Donald R Gauthier

Hongming Li

Rebecca T Ruck

The application is directed to efficient and economical processes as described in more detail below for the preparation of the beta 3 agonists of the formula of I-7 and intermediate compounds that can be used for making these agonists. The present disclosure relates to a process for making beta-3 agonists and intermediates using ketoreductase (KRED) biocatalyst enzymes and methods of using the biocatalysts.

Process for preparing beta 3 agonists and intermediates

The application is directed to efficient and economical processes as described in more detail below for the preparation of the beta 3 agonists of the formula of I-7 and intermediate compounds that can be used for making these agonists. The present disclosure relates to a process for making beta-3 agonists and intermediates using ketoreductase (KED) biocatalyst enzymes and methods of using the biocatalysts.

The present invention includes compounds useful as intermediates in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing macrolactams. One use of the methods and intermediates described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity. HCV NS3 inhibitory compounds have therapeutic and research applications.

Methods and intermediates for preparing macrolactams

The present invention is directed to processes for the preparation of 4-(3-methanesulfonyl-phenyl)-1-N-propylpiperidine (I) or a pharmaceutically acceptable salt thereof, which comprises: oxidizing a sulfide of the formula (II): with a catalytic oxidizing agent and an oxidant; to give a compound of the formula (III): followed by catalytic reduction of the compound of formula (III).

Process for the synthesis of 4-(3-methanesulfonylphenyl)-1-N-propyl-piperidine

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Readington, NJ, United States of America

Richard Desmond