Merck Sharp + Dohme Corp.

Msd R&d Cn Co., Ltd

Tetsuji Itoh

Kevin Campos

Kevin Michael Belyk

Gang Qian

Jingjun Yin

Donald R Gauthier

Yang Cao

Benjamin D Sherry

Feng Xu

David M Tschaen

Guy R Humphrey

Richard John Varsolona

John Y L Chung

Zhuqing Liu

Artis Klapars

Edward Cleator

Jianguo Yin

Jeremy Peter Scott

Andrew William Gibson

Alexei Kalinin

Michel Journet

Ji Qi

Yonggang Chen

Ian Mangion

Ingyu Jeon

Qinghao Chen

Bangping Xiang

Louis-Charles Campeau

Alan Michael Hyde

Wensong Xiao

Jungchul Kim

Hongming Li

Debra J Wallace

Andrew Brunskill

Aaron M Dumas

Melodie Deniz Christensen

Matthew Thomas Tudge

Jacob Henry Waldman

Andrew Wood

The invention is related to the preparation of protected piperidine carboxylates suitable for use as intermediates that lead, via a series of additional process steps, including a sulfation of a hydroxy urea compound, to the preparation of the beta lactamase inhibitor (2S,5R)-7-oxo-N-piperidin-4-yl-6-(sulfoxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide.

Process for the preparation of intermediates useful for making (2S,5R)-7-oxo-n-piperidin-4-yl-6-(sulfoxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide

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

The present invention is directed to a process for making Tetracyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein X, X, R, Rand Rare defined above herein. The present invention is also directed to compounds that may be useful as synthetic intermediates in the process of the invention.

Process for making tetracyclic heterocycle compounds

The present invention is directed to a novel process for synthesizing 3-(substituted phenoxy)-1-[(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methyl])-pyridin-2(1H)-one derivatives. The compounds synthesized by the processes of the invention are HIV reverse transcriptase inhibitors useful for inhibiting reverse transcriptase, HIV replication and the treatment of human immunodeficiency virus infection in humans.

Process for making reverse transcriptase inhibitors

The present invention is directed to a novel process for synthesizing 3-(substituted phenoxy)-1-[(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methyl])-pyridin-2(1H)-one derivatives. The compounds synthesized by the processes of the invention are HIV reverse transcriptase inhibitors useful for inhibiting reverse transcriptase and HIV replication, and the treatment of human immunodeficiency virus infection in humans.

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Somerset, NJ, United States of America

Tetsuji Itoh