Schering Corporation

Merck Sharp + Dohme Corp.

Werthenstein Biopharma Gmbh

Tao Wang

William J Greenlee

Samuel Chackalamannil

Tiruvettipuram K Thiruvengadam

Jing Liao

Anantha R Sudhakar

George G Wu

Mingsheng Huang

Ngiap Kie Lim

Daw-long Albert Kwok

Frank Xing Chen

Marc Poirier

Xiaojing Yang

John S Chiu

Hoa N Nguyen

Ji Xie

Ilia A Zavialov

Michael D Green

Feng Xu

Wenxue Wu

Guy R Humphrey

Xiaoyong Fu

Zhiguo Jake Song

Hong-Chang Lee

Laura Marie Artino

Xin Wang

Richard John Varsolona

Yong-Li Zhong

Jeonghan Park

Tao Pei

Lu Chen

Ji Qi

Michael P Graziano

Jian Cui

Vijay Sabesan

Daw-Iong Albert Kwok

David Jieh-Shyh Tsai

Richard Desmond

Jungchul Kim

David J S Tsai

Clinton Scott Shultz

Teng Li

Hongming Li

Rebecca T Ruck

Teddy Kosoglou

Zhiwei Chen

Taotao Lu

Patrick Larpent

Jianjun Duan

Kangze Dai

Nastaran Salehi Marzijarani

Het P Patel

Haiheng Guo

Madhu Chintala

Eric M Phillips

Joshua Lee

Chintal Desai

Stephen M Dalby

Illia Zavialov

Anastasia Pavlovsky

Ngiap-Kie Lim

Vijay Sabesen

Susan Bogdanowich-Knipp

Daw-Long Kwok

Ilia Zavialov

The disclosure provides crystalline forms for certain synthetic intermediates for making belzutifan, a HIF-2&#x3b1; inhibitor, useful for the treatment of cancer. The disclosure also provides processes for isolating the crystalline forms.

Synthetic pathway to belzutifan and crystalline phases of synthetic intermediates

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 includes compounds useful as intermediates in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing macrolactams from the intermediates. 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.

Process and intermediates for preparing macrolactams

This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center. The chemistry taught herein can be exemplified by the following: 

Exo- and diastereo-selective synthesis of himbacine analogs

This application discloses a novel process for the synthesis of himbacine analogs, as well as the compounds produced thereby. The synthesis proceeds by alternative routes including the cyclic ketal amide route, the chiral carbamate amide route, and the chiral carbamate ester route. The compounds produced thereby are useful as thrombin receptor antagonists. The chemistry disclosed herein is exemplified in the following synthesis sequence: 

Exo-selective synthesis of himbacine analogs

Exo- and diastereo- selective synthesis of himbacine analogs

Exo- and diastereo-selective syntheses of himbacine analogs

This application discloses provides a process for the introduction of nitro-group functionality into a compound which contains also a site of unsaturation and/or oxygen functionality by direct (one step) oxidation of an oxime functional group mediated by a molybdenum VI/VII peroxo complex, the process comprising:  Where Rand Rare as defined above.

Synthesis of 3-(5-nitrocyclohex-1-enyl) acrylic acid and esters thereof

The present invention relates to an improved process for preparing himbacine analogs. The compounds are useful as thrombin receptor antagonists. The improved process may allow for at least one of easier purification by crystallization, easier scalability, and improved process yield on the desired enantiomer. An example of a step in the synthesis of such a himbacine analog is as follows: 

Synthesis of himbacine analogs

Exo- and diastereo- selective syntheses of himbacine analogs

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Springfield, NJ, United States of America

Tao Wang