An improved synthesis of TRβ-selective thyromimetic GC-1

TRβ选择性甲状腺拟甲状腺素GC-1的改进合成

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Abstract

A new efficient synthesis of TR(β)-selective thyromimetic GC-1 is described. The present strategy employs benzyl substituent as the exclusive protecting group, avoiding side reactions and simplifying the purification process in the last step. This paper reports 62% overall yield in six steps for total synthesis of GC-1 in multi-gram scale. The initial synthetic route is adaptable to analogue design and suitable for the preparation of other natural methylenebisphenols.

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