一种来那度胺的合成方法

Method for synthesizing lenalidomide

Abstract

一种来那度胺的合成方法,本发明属于有机合成中的抗肿瘤及白血病类药物合成领域,具体涉及一种合成来那度胺的方法。本发明为了解决传统来那度胺合成反应中收率低、纯度低、产生大量有害废物污染环境、环保治理成本过高、易发生剧烈爆炸产生危险、高温下反应时间长造成降解、催化剂回收套用次数低的问题。方法:一、将来那度胺前体硝基物加入到有机溶剂中,再加入Pd负载量为10%的活性炭催化剂后,将混合物作为物料I进入微通道反应器的预热模块;二、物料I预热后与物料II氢气分别打入微通道反应器的反应模块组反应,收集流出的反应液,处理得到来那度胺。本发明绿色环保、反应收率高、纯度高、经济性好。
The invention provides a method for synthesizing lenalidomide, belongs to the field of anti-tumor and anti-leukemia medicines in organic synthesis, and particularly relates to the method for synthesizing lenalidomide. To solve the problems of low yield, low purity, environmental pollution caused by massive harmful waste, excessive cost for environment-friendly treatment, easily occurred risk of violent explosive, degradation caused by long reacting time at high temperature and low catalyst recycling frequency in a traditional lenalidomide synthesis reaction, the method comprises the following steps: 1, adding a lenalidomide precursor nitro compound into an organic solvent, adding an activated carbon catalyst having a Pd loading capacity of 10 percent, then leading the mixture serving as a material I into a pre-heating module of a microchannel reactor; and 2, respectively pumping preheated material I and a material II hydrogen into a reaction module of the microchannel reactor into a reactor, collecting outflowing reaction liquid, and treating to obtain the lenalidomide. The method is environment-friendly, and has the advantages of high reaction yield, high purity and good economical efficiency.

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