Invention Grant
US07687631B2 Synthesis of diethyl{[5-(3-fluorophenyl)-pyridine-2yl]methyl}phosphonate
有权
{[5-(3-氟苯基) - 吡啶-2-基]甲基}膦酸二乙酯的合成
- Patent Title: Synthesis of diethyl{[5-(3-fluorophenyl)-pyridine-2yl]methyl}phosphonate
- Patent Title (中): {[5-(3-氟苯基) - 吡啶-2-基]甲基}膦酸二乙酯的合成
-
Application No.: US11824245Application Date: 2007-06-29
-
Publication No.: US07687631B2Publication Date: 2010-03-30
- Inventor: Kelvin H. Yong , Ilia A. Zavialov , Jianguo Yin , Xiaoyong Fu , Tiruvettipuram K. Thiruvengadam
- Applicant: Kelvin H. Yong , Ilia A. Zavialov , Jianguo Yin , Xiaoyong Fu , Tiruvettipuram K. Thiruvengadam
- Applicant Address: US NJ Kenilworth
- Assignee: Schering Corporation
- Current Assignee: Schering Corporation
- Current Assignee Address: US NJ Kenilworth
- Agency: Patent Practitioners of Schering Corp.
- Agent H. Eric Fischer
- Main IPC: C07D405/06
- IPC: C07D405/06
![Synthesis of diethyl{[5-(3-fluorophenyl)-pyridine-2yl]methyl}phosphonate](/abs-image/US/2010/03/30/US07687631B2/abs.jpg.150x150.jpg)
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 R9 is selected from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms, and R11 is selected independently for each occurrence from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms and hydrogen, X2 is Cl, Br, or I; X3 is selected from Cl and Br; and PdLn is 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.
Public/Granted literature
- US20080004449A1 Synthesis of diethyl{[5-(3-fluorophenyl)-pyridine-2yl]methyl}phosphonate Public/Granted day:2008-01-03
Information query