3-(2-甲氧基-5-甲基苯基)-3-苯丙醇的合成

Synthesis of 3-(2-Methoxy-5-methylphenyl)-3-phenylpropanol

对甲苯酚和肉桂酸经脱水环合、水解甲基化制得3-(2-甲氧基-5-甲基苯基)-3-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托特罗定中间体3-(2-甲氧基-5-甲基苯基)-3-苯丙醇,总收率89%。

3-（2-Methoxy-5-methylphenyl）-3-phenylpropanol, the important intermediate of tolterodine was synthesized from p-cresol and cinammic acid by dehydration, cyclization, hydrolysis and methylation to give 3- （2-methoxy-5-methylphenyl） -3-phenylpropionic acid, which was subjected to reduction by NaBHn/BF3 · Et20 with an overall yield of 89 %.