对硝基苯磺酰基乙酸酯的二烷基化反应

A FACILE DIALKYLATION OF P-NITROPHENYL SULFONYL ACETATES

对硝基苯磺酰基乙酸酯(1_a—e)在固-液相转移催化条件下,可以进行烷基化反应生成二烷基化产物。1_a—e中苯环上的硝基使反应活性增加,多种类型的烷基化试剂,如溴乙烷、溴丙烯和氯苄均可与其反应得到烷基化产物。本文中合成了18种二烷基化产物。4-O_2NC_6H_4SO_2CR^1R^2CO_2R(2a—i,3a—i)。方法的优点是反应条件温和,产率高(88—98％)。

This paper reports a facile dialkylation of p-nitrophenylsulfonylacetates (1_(a-e)) under solid-liquid phase transfer conditions. The reactivity of the substrates is increased by the nitro group in benzene ring. A variety of alkylating agents, such as ethyl bromide, allyl bromide and bcnzyl chloride, can be used to transform with 1 to the corresponding alkylated products in good to excellent yields. Eighteen dialkylated compounds (2a-i, 3a-i) have been synthesized and characterized. This method has the advantage of moderate reaction conditions and hizh yields.