The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Mar. 30, 2010
Filed:
Jun. 29, 2007
Kelvin H. Yong, Lyndhurst, NJ (US);
Ilia A. Zavialov, Princeton, NJ (US);
Jianguo Yin, Plainsboro, NJ (US);
Xiaoyong Fu, Edison, NJ (US);
Tiruvettipuram K. Thiruvengadam, Kendall Park, NJ (US);
Kelvin H. Yong, Lyndhurst, NJ (US);
Ilia A. Zavialov, Princeton, NJ (US);
Jianguo Yin, Plainsboro, NJ (US);
Xiaoyong Fu, Edison, NJ (US);
Tiruvettipuram K. Thiruvengadam, Kendall Park, NJ (US);
Schering Corporation, Kenilworth, NJ (US);
Abstract
This application discloses a novel process for the preparation of phosphonate esters useful as intermediates in the preparation of himbacine analogs, themselves useful as thrombin receptor antagonists. The chemistry taught herein can be exemplified by the following scheme: wherein Ris selected from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms, and Ris selected independently for each occurrence from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms and hydrogen, Xis Cl, Br, or I; Xis selected from Cl and Br; and PdLis a supported palladium metal catalyst or a soluble heterogeneous palladium catalyst. The L-derivatizing reagent is a moiety which converts the alcohol functional group of compound 137D to any leaving group which can be displaced by a triorgano-phosphite phosphonating agent.