1-甲基-1H-吡唑-5-硼酸频哪醇酯的合成  

Synthesis of Pinacol 1-Methyl-1H-pyrazole-5-boronate

作　　者：张玉娟[1] 邢磊[1] 陈国良[1] 

机构地区：[1]沈阳药科大学基于靶点的药物设计与研究教育部重点实验室,辽宁沈阳110016

出　　处：《精细化工中间体》2013年第6期27-28,58,共3页Fine Chemical Intermediates

摘　　要：以1H-吡唑为原料,经磷酸三甲酯甲基化,正丁基锂锂化后与硼酸三甲酯硼酸化,再与频哪醇缩合得到1-甲基1H-吡唑-5-硼酸频哪醇酯,3步反应的总收率为27.4%。优化了中间体3的合成和纯化。目标化合物经1H NMR结构确证。1-Alkyl-pyrazole acid is an important intermediate for the synthesis of many biologically active compounds. The target compound was prepared in overall yield of 27.4% starting from 1H-pyrazole via methylation with trimethy｜ phosphate,converting into boronic acids with trimethyl borate after reaction with n- butyl lithium,and condensation with pinacol. The process conditions were optimized for the synthesis and purification of intermediate 3. The structure of target compound was characterized by IH NMR.

关 键 词：1-甲基-1H-吡唑-5-硼酸频哪醇酯 合成 频哪醇 

分 类 号：TQ463[化学工程—制药化工] Q624.32[生物学—生物物理学]