瑞他莫林的合成

Synthesis of Retapamulin

内-8-甲基-8-氮杂二环[3.2.1]辛烷-3-甲磺酸酯与N,N-二乙基二硫代氨基甲酸钠三水合物反应得外-8-甲基-8-氮杂双环[3.2.1]辛-3-基-N,N二乙基氨基二硫代甲酸酯,经水解后,与截短侧耳素-22-甲磺酸酯缩合得抗菌药瑞他莫林,总收率45.9%。

Retapamulin was prepared in a total yield of 45.9% by nucleophilic substitution of endo-8-methyl-8-azabicyclo[3.2.1]octan-3-yl methanesulfonate and sodium N,N-diethyldithiocarbamate trihydrate to give exo-8-methyl-8-azabicyclo[3.2.1]octan-3-yl N,N-diethyldithiocarbamate, followed by hydrolysis and condensation with pleuromutilin-22-mesylate.