右旋布比卡因消旋化研究

Racemization of (R)-(+)-Bupivacaine

考察了(R)-(+)-布比卡因消旋化的方法和条件。以消旋产物中(S)-(-)-布比卡因的含量为指标,采用乙二醇/水为消旋试剂,通过单因素试验考察消旋试剂用量、消旋温度、反应时间等因素对(R)-(+)-布比卡因消旋效果的影响。以乙二醇-水(9︰1)为消旋试剂,与(R)-(+)-布比卡因的比例为6︰1(v/w),140℃反应2h,消旋产物中(S)-(-)-布比卡因含量为42.2%。

The racemization of （R） - （＋） -bupivacaine was discussed and the racemization effects were evaluated with the content of （S）- （-）-bupivacaine in racemization mixture as the index. The influences of reaction temperature, reaction time and solvent amount on racemization were investigated by single factor test. The content of （S）-（-）- bupivacaine in the end product of reaction was 42.2% in ethylene glycol-water （9： 1） at ratio of 1 ： 6 （w/v） for 2 h at 140 ℃.