Schüttler A, Brandenburg D
Hoppe Seylers Z Physiol Chem. 1979 Dec;360(12):1721-5.
The preparation of N,N-bis(methylsulfonylethoxycarbonyl)insulins is described. In an aequeous buffer at pH 5.8 selectivity of the reaction of insulin with 20 equivalents of N-(methysulfonylethoxycarbonyloxy)succinimide (Msc-ONSu) leads very specifically to N alpha A 1,-N alpha B 1-(Msc)2 - insulin. The product can be isolated in a yield of 60%. Using N alpha A 1-citraconylinsulin the N alpha B 1, NEB29-(Msc)2 -insulin can be prepared in a yield of 40% based on insulin.
本文描述了N，N-双（甲基磺酰基乙氧基羰基）胰岛素的制备方法。在pH值为5.8的水性缓冲液中，胰岛素与20当量的N-（甲基磺酰基乙氧基羰基氧基）琥珀酰亚胺（Msc-ONSu）反应具有选择性，可非常特异性地生成NαA1，-NαB1-（Msc）2-胰岛素。该产物的分离产率可达60%。以NαA1-柠康酰胰岛素为原料，基于胰岛素的产率为40%，可制备出NαB1，NεB29-（Msc）2-胰岛素。
