Schering Corporation

Knopp Biosciences, LLC

Merck Sharp + Dohme Corp.

Daw-Iong Albert Kwok

Anantha R Sudhakar

Tiruvettipuram K Thiruvengadam

George G Wu

Frank Xing Chen

Xiaoyong Fu

Marc Poirier

Minzhang Chen

Xiaojing Yang

Ilia A Zavialov

Jeonghan Park

Tao Wang

Chou-Hong Tann

Michael J Humora

George S Wong

Michael D Green

Hoa N Nguyen

William F Kiesman

Jing Liao

Ji Xie

Weirong Chen

Erwin Irdam

Eugene John Vater

Mingsheng Huang

Ngiap Kie Lim

Jian Cui

Juergen Weber

Weidong Tong

Ingyu Jeon

Ramani R Raghavan

Vijay Sabesan

Maria M Tamarez

David J Tsai

The present invention is related to an improved process for the preparation of amino-substituted 4,5,6,7-tetrahydrobenzothiazole compounds of formula I, such as the compound 2-amino-4,5,6,7-tetrahydro-6-(n-propylamino)benzothiazole. The invention further relates to an improved synthesis of (R)-2-amino-4,5,6,7-tetrahydro-6-(n-propylamino)benzothiazole. The invention also relates to the methods and intermediates associated with the synthetic process.

Synthesis of amine substituted 4,5,6,7-tetrahydrobenzothiazole compounds

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

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 syntheses of himbacine analogs

The invention provides an improved process for the preparation of 17-esters of 9.alpha.,21 -dihalo-pregnane-11.beta.,17.alpha.-diol-20-ones, and in particular for the preparation of 17-esters of anti-inflammatory steroids according to the following scheme: ##STR1## wherein RCO, R.sup.1, X, Y and the dotted line are as defined in the specification. The novel process is especially suitable for the preparation of Mometasone Furoate.

Process for the preparation of 17-esters of 9 .alpha.,

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Gillette, NJ, United States of America

Daw-Iong Albert Kwok