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抗心律失常和局部麻醉药物利多卡因(Lidocain)的生产,国内都采用间-二甲苯为原料,先经硝化反应合成中间体2-硝基-1,3-二甲苯。但由于受空间位阻等因素的影响,间-二甲苯的硝化反应,硝基主要进入间-二甲苯的4-位,在硝化产物中75%为4-硝基1,3-二甲苯,生产利多卡因所需的中间体2-硝甚-1,3-二甲苯仅占25%。在实际生产中,由于各种条件的影响,副产物4-硝基-1,3-二甲苯所占比例往往超过文献指标,一般占硝基物总量的80~
Anti-arrhythmia and local anesthetic drugs Lidocain production, the domestic use of m-xylene as raw material, the first by nitration synthesis of 2-nitro-1,3-dimethylbenzene. However, due to steric hindrance and other factors, the nitration of m-xylene mainly enters the 4-position of m-xylene and 75% of the nitration product is 4-nitro-1,3-dimethylbenzene. The intermediate 2-nitro-1,3-xylene required for the production of lidocaine accounted for only 25%. In actual production, due to the influence of various conditions, the proportion of by-product 4-nitro-1,3-dimethylbenzene often exceeds the literature index, generally accounting for 80 ~