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Preparation of n n bis methylsulfonylethoxycarbonyl insulins

, : Preparation of n n bis methylsulfonylethoxycarbonyl insulins. Hoppe-Seyler's Zeitschrift fuer Physiologische Chemie 360(12): 1721-1726

The preparation of N,N-bis(methylsulfonylethoxycarbonyl)insulins is described. In an aqueous buffer at pH 5.8 selectivity of the reaction of insulin with 20 equivalents of N-(methylsulfonylethoxycarbonyloxy)succinimide (Msc-ONSu) leads very specifically to N.alpha.A1, N.alpha.B1-(Msc)2-insulin. The product can be isolated with a 60% yield. Using N.alpha.A1-citraconylinsulin the N.alpha.B1,N.epsilon.B29-(Msc)2-insulin can be prepared with a 40% yield based on insulin.

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