盐酸西布曲明的合成

Synthesis of Sibutramine Hydrochloride

以对氯氯苄为原料 ,经取代、环合、加成、还原、二甲基化及成盐等反应合成盐酸西布曲明。还原反应改用成本较低的硼氢化钾 ;二甲基化反应改用条件温和、对环境污染少的甲醛 -硼氢化钾系统 ,使该步收率可达 92 %。方法操作简便 ,条件温和 ,成本较低 ,总收率 44 % (以 2计 )

Sibutramine hydrochloride, a new drug for treating obesity, was synthesized by substitution of 4 chlorobenzyl chloride with NaCN/CH 3OH, cyclization, addition, reduction, dimethylation and then salt formation in an overall yield of 36.6%.