3-(2-甲氧基-5-甲基苯基)-3-(4-甲基)-苯丙醇的合成

Synthesis of 3-(2-methoxy-5-methylphenyl)-3-(4-methyl)-phenylpropanol

目的:合成新型托特罗定类似物中间体。方法:对甲苯酚和4-甲基肉桂酸经脱水环合、水解甲基化制得3-(2-甲氧基-5-甲基苯基)-3-(4-甲基)-苯丙酸,用硼氢化钠在三氟化硼乙醚复合物作用下以无水THF为溶剂直接还原制得新型托特罗定类似物中间体3-(2-甲氧基-5-甲基苯基)-3-(4-甲基)-苯丙醇。结果:总收率79.07%。结论:合成新型托特罗定类似物中间体,合成路线利于工业化生产。

Objective ： To synthesis new intermediates of tolterodine analogues. Methods ~ 3- （2-methoxy- 5-methylphenyl）- 3-（4-methyl）-phenylpropanol, the new intermediate of analogue of tolterodine was synthesized from p-cresol and 4-methyl cinammic acid by dehydration, cyclization, hydrolysis and methylation to give 3-（2-methoxy-5-methylphenyl）- 3-（4-methyl）-phenylpropanol acid, which was subjected to reduction by NaBH4/BF Et2O. Result：The total yield was 79.07 %. Conclusion：To synthesis new intermediates of tolterodine analogues, synthetic route is conductive to industrial production.