A METHOD FOR PREPARATION OF SIBUTRAMINE SULFONATE SALT AND A COMPOSITION CONTAINING THE SAME FOR TREATING AND PREVENTING OBESITY DISEASE

摘要

A sibutramine sulfonate salt is provided to obtain a pharmaceutically active ingredient useful for preventing or treating obesity or obesity-related diseases and having excellent solubility, stability, hygroscopic property, shelf life and bioavailability. A sibutramine sulfonate salt is represented by the following formula I, wherein A is OR2 or NR3R4, R1 is a hydrogen atom or methyl group, R2 is a C1-C5 alkyl group, and each of R3 and R4 independently represents a hydrogen atom or a C1-C5 alkyl group, or R3 and R4 are linked to each other to form a 5-membered or 7-membered cyclic alkyl group. The sibutramine sulfonate is obtained by reacting sibutramine with a reagent containing an alkoxy group and a sulfonyl group in an organic solvent.