首页> 外国专利> SYNTHESIS OF DIERHYL{15'(3-FLUOROPHENYL)-PYRIDINE-2-YLMETHYL}PHOSPHONATE USED IN THE SYNTHESIS OF HIMC=BACINE ANALOGS

SYNTHESIS OF DIERHYL{15'(3-FLUOROPHENYL)-PYRIDINE-2-YLMETHYL}PHOSPHONATE USED IN THE SYNTHESIS OF HIMC=BACINE ANALOGS

机译:用于合成HIMC = BACINE类似物的二{15“(3-氟苯基)-吡啶-2-基]甲基}磷酸二酯

摘要

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.
机译:该申请公开了一种制备膦酸酯的新方法,该膦酸酯用作制备组氨酸类似物的中间体,其本身可用作凝血酶受体拮抗剂。本文所教导的化学反应可以通过以下方案例示:其中R 9选自具有1至10个碳原子的烷基,芳基杂芳基和芳基烷基,并且R 11每次独立地选自具有1至10个碳原子的烷基,芳基杂芳基和芳基烷基。 10个碳原子和氢,X 2为Cl,Br或I; X3选自Cl和Br; PdLn是负载型钯金属催化剂或可溶性多相钯催化剂。 L-衍生化试剂是将化合物137D的醇官能团转化为可被三有机亚磷酸酯膦酸酯化的任何离去基团的部分。

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