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AN IMPROVED PROCESS FOR THE PREPARATION OF INTERMEDIATE OF LEUKOTRIENE RECEPTOR ANTAGONIST

机译:一种改进的制备白三烯受体拮抗剂的中间体的方法

摘要

ABSTRACT: The present invention relates to a process synthetic process for preparing the side-chain precursor l- (mercaptomethyl)cyclopropancacctic acid, Which is useful in the synthesis of leukotriene receptor antagonist such as Montelukast and salts thereof. Preferably the present invention relates to a process for the prepartion of 1- (bromomethyl) Cyclopropane-acetonitrile starting from 1- (hydroxymethyl)cyclopropaneacetonitrile. Preferably, the present invention relates to avoiding the use of toxic solvent such as DMF and additional component such asr sodium iodide in the preparation ofl-(hydroxymethyl)cyclopropaneacetonitrile. Preferably, the present invention relates avoding the use of reagents PBr3 or Ph3P/Br2in the preparation of l-(bromomethyl) Cyclopropane-acetonitrile.
机译:摘要:本发明涉及制备侧链前体1-(巯基甲基)环丙酸的方法的合成方法,该方法可用于白三烯受体拮抗剂如孟鲁司特及其盐的合成。优选地,本发明涉及从1-(羟甲基)环丙烷乙腈开始制备1-(溴甲基)环丙烷-乙腈的方法。优选地,本发明涉及在制备1-(羟甲基)环丙烷乙腈中避免使用有毒溶剂例如DMF和另外的组分例如碘化钠。优选地,本发明涉及在制备1-(溴甲基)环丙烷-乙腈中使用试剂PBr3或Ph3P / Br2。

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