Merck Sharp + Dohme Corp.

Merck + Co., Inc.

Jeffrey T Kuethe

Jacob M Janey

Robert F Dunn

Lushi Tan

Jeremy Peter Scott

Michael J Zacuto

Faye Sheen

David R Lieberman

Qinghao Chen

Aaron J Moment

Nadine Bremeyer

Nobuyoshi Yasuda

Guy R Humphrey

Mark A Huffman

Yong-Li Zhong

Edward Cleator

Gregory L Beutner

Michel Journet

Jingjun Yin

Carl A Baxter

A process for the preparation of pyrazolopyrolidines of structural formula I: and W is or P, wherein in P is an amine protecting group. These compounds are useful in the synthesis of dipeptidyl peptidase-IV inhibitors for the treatment of Type 2 diabetes. Also provided are useful intermediates obtained from the process.

Process for preparing chiral dipeptidyl peptidase-IV inhibitors

A process for the preparation of pyrazolopyrolidines of structural formula I: and W is or P, wherein in P is an amine protecting group. These compounds are useful in the synthesis of dipeptidyl peptidase-IV inhibitors for the treatment of Type 2 diabetes. Also provided are useful intermediates obtained from the process. 

A first aspect of the present invention describes a compound selected from group consisting of: wherein R is either H, C(O)R, or C(O)NHCH(X)COOH; provided that X is a C-Calkyl, or a C-Ccycloalkyl and Ris a Calkyl or aryl; These compounds are used to make Compound A 

Methods and intermediates for preparing macrolactams

The present invention is directed to a process for preparing certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The compounds are useful in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.

Process for making hydroisoindoline tachykinin receptor antagonists

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Somerset, NJ, United States of America

Jeffrey T Kuethe