Oelschläger H, Iglesias-Meier J, Götze G, Schatton W
Arzneimittelforschung. 1977;27(9):1625-8.
4-[3-(4-phenoxymethyl-phenyl)-propyl]-morpholine (fomocaine, Erbocain) is a very active topical local anaesthetic with low toxicity. A new synthesis starting from 4-phenoxy-methyl-benzonitrile, via a modified Willgerodt-Kindler reaction, is reported. The yield is of the same order as with the known technical process starting from 3-phenylpropanol. The distinct advantage of the new procedure is the avoidance of the C-chloromethylation of 3-phenylpropylchloride during which process the o-chloromethyl derivative is also formed, and this cannot be separated by fractional distillation.
4-[3-(4-苯氧甲基苯基)丙基]吗啉(福莫卡因,厄波卡因)是一种活性很强的局部外用麻醉剂,毒性较低。本文报道了一种以4-苯氧甲基苯腈为起始原料,通过改进的威尔格罗德特-金德勒反应进行的新合成方法。其产率与从3-苯基丙醇开始的已知工业方法相当。新方法的显著优点是避免了3-苯基丙基氯的碳氯甲基化过程,在此过程中还会形成邻氯甲基衍生物,且无法通过分馏分离。