Merck Sharp + Dohme Corp.

Clariant Corporation

Archimica Gmbh

Alexei Kalinin

Zhuqing Liu

Feng Xu

Birgit Kosjek

Hongmei Li

Hallena Strotman

Jeonghan Park

Richard Desmond

Johannah R Moncecchi

Stefan Scherer

Victor Snieckus

Richard John Varsolona

Andreas Meudt

Kevin Campos

Jianguo Yin

Kevin Michael Belyk

Jingjun Yin

Bangping Xiang

Tetsuji Itoh

Andrew Brunskill

Melodie Deniz Christensen

Guofang Qiu

Thomas J Marren

James E Aldred, Jr

Yu Ji

Bernd Lehnemann

Jr Aldred

Jr James E Aldred

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 is directed to processes for preparing Substituted Tetracyclic Heterocycle Compounds of formula (I): (I) which may be useful as HCV NS5A inhibitors. The present invention is also directed to compounds that may be useful as synthetic intermediates and catalysts in the processes of the invention. 

Process for preparing substituted tetracyclic heterocycle compounds

A process for preparing the d-threo isomer of methylphenidate hydrochloride which includes (i) resolving a racemic mixture of racemic threo-methylphenidate hydrochloride with a less than stoichiometric amount of tertiary amine base to obtain a methylphenidate-chiral acid salt, (ii) basifying the methylphenidate-chiral acid salt to obtain methylphenidate free base, and (iii) converting the methylphenidate free base into d-threo-methylphenidate hydrochloride.

Process of enantiomeric resolution of D,L-(&#xb1;)-threo-methylphenidate

A process for preparing anilineboronic acid derivative of the formula I, by converting an aniline to a diprotected aniline by introducing two protecting groups, metalating the diprotected aniline with a metalating agent and simultaneously or subsequently reacting with a boronic ester B(OR)to form a protected anilineboronic ester, which is converted, by detaching the protecting groups, to the anilineboronic esters of the formula (I).

Preparation of Anilineboronic acids and derivatives thereof

A process for preparing bisallylboranes of the formula (I) by reacting a diene with sodium borohydride in the presence of an oxidant:in an inert solvent, with the borane generated in situ reacting selectively with the diene to form the bis(allyl)borane of the formula (I) and the substituents Rto Rhaving the following meanings: As oxidant, it is possible to use, for example, alkyl halides or dialkyl sulfates. In a particularly preferred embodiment, the diene used is 2,5-dimethylhexa-2,4-diene (R, R, R, R=methyl, R, R=H).

Process for preparing bisallylboranes and nonaromatic boronic acids

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Morganville, NJ, United States of America

Alexei Kalinin