Study on the regioselective alkylation of 2-thiopyrimidine  

选择性合成2-硫嘧啶烷基取代产物(英文)

作　　者：徐杨[1] 杨华[1] 胡晋[1] 王孝伟[1] 刘俊义[1] 

机构地区：[1]北京大学药学院化学生物学系

出　　处：《Journal of Chinese Pharmaceutical Sciences》2007年第2期125-127,共3页中国药学（英文版）

基　　金：National Nature Science Foundation of China(NO.20172007).

摘　　要：Aim To investigate the alkylation of 2-thiopyrimidine. Methods Treating the starting material 2-thiopyrimidine with chloromethyl ethers via a procedure of K2CO3 in DMF or with alkyl halide in CH3ONa-CH3OH at room temperature, to obtain the corresponding regioselective 2-S-allkyl pyrimidines. The products were determined by JH NMR, 2D NMR, IR and MS spectra. Results 2-S-alkyl-pyrimidines were regioselectively synthesized. Conclusion In different conditions with different alkyl halides, 2- thiouracil could be converted into the corresponding 2-S-alkylpyrimidines regioselectively.目的研究2-硫嘧啶S上烷基取代反应。方法以2-硫嘧啶为原料,分别采用K2CO3方法和CH3ONa-CH3OH方法,合成了2位硫烷基取代产物。采用1H NMR,IR,质谱鉴定了产物。结果高度区域选择性地、以较好的收率得到了2位硫烷基取代产物。结论CH3ONa-CH3OH方法可以高度区域选择性地合成2位硫烷基取代产物,而K2CO3方法得到多取代烷基化产物。

关 键 词：ALKYLATION 2-Thio-6-methyl-uracil 2-Alkylthiopyrimidine 6-Methyl-3  4-dihydro-2H-pyfido [2  l-b] [ 1  3] thiazin-8-one 

分 类 号：R914[医药卫生—药物化学]