非索非那定的合成

Synthesis of Fexofenadine

α,α-二甲基苯乙酸经硅胶负载磷钨酸(PW/SiO2)固体酸催化酯化、与4-氯丁酰氯反应生成α,α-二甲基-4-(4-氯-1-氧代丁基)苯乙酸乙酯,用硼氢化钠还原后与α,α-二苯基-4-哌啶甲醇反应、碱性水解制得抗组胺药非索非那定,总收率约48%。

Fexofenadine, an antihistaminic drug, was synthesized from α,α-dimethylbenzeneacetic acid via PW/ SiO2 catalytic esterification, acylation, reduction, reaction with α,α-diphenyl-4-piperidine methanol and then hydrolysis with an overall yield of about 48 %.