(4-甲氧基-3-硝基苄磺酰基)乙酸的制备

取代的苄磺酰基乙酸类化合物可用于合成多种抗肿瘤药~([1,2]).其中(4-甲氧基-3-硝基苄磺酰基)乙酸(1)可用于合成Polo-like激酶1抑制剂类抗肿瘤药novonex(ON-01910),文献~([1,2])用4-甲氧基-3-硝基溴(氯)苄和巯基乙酸缩合得(4-甲氧基-3-硝基苄硫基)乙酸(2),再用过氧羧酸(如过氧乙酸)在回流条件下氧化,反应结束后蒸去溶剂得1,但由于存在过氧酸容易发生爆炸.

Preparation of (4-Methoxy-3-nitrobenzylsulfonyl) acetic Acid

(4-Methoxy-3-nitrobenzylsulfonyl) acetic acid was prepared from 4-methoxy-3-nitrobenzyl bromide by condensation with thioglycolic acid, and then oxidation with H_2O_2 in presence of Na_2WO_4 with an overall yield of about 71%.