KANG Fang-yuan1,2, PANG Xue-hai1,2, WANG Ying-wei1,2, CHEN Yuan-wei1,3
1. Chengdu Institute of Organic Chemistry, Chinese Academy of Sciences, Chengdu 610041, China; 2. University of Chinese Academy of Science, Beijing 100049, China; 3. State Key Labboratory of Biotheraphy, Sichuan Univeristy, Chengdu 610041, China
Abstract：The synthesis of deuterated AZD9291 was reported. 3-(2-Chloropyrimidin-4-yl)-1H- indole(1) was prepared by coupling reaction of indole with 2,4-dichloropyrimidine. 3-(2-Chloropyrimidin-4-yl)-1-(methyl-d3)-lindole(2) was obtained by substitution reaction of 1 with iodomethane-d3. N′-(2-dimethylaminoethyl)-2-methoxy-N′-methyl-N-{［4-(1- methyl-d3)indol-3-yl］pyrimi- din-2-yl}benzene-1,2,4-triamine(4) was obtained by two substitution reactions from 2. Then deuterated AZD9291 in total yield of 8.5% was synthesized by condensation reaction following reduction of 〖STHZ〗4〖STBZ〗. The structures were confirmed by 1H NMR, 13C NMR and ESI-MS.
康芳圆， 庞学海， 王颖伟， 陈元伟. 氘代AZD9291的合成[J]. 合成化学, 2016, 24(3): 263-265.
KANG Fang-yuan, PANG Xue-hai, WANG Ying-wei, CHEN Yuan-wei. Synthesis of Deuterated AZD9291. Chinese Journal of Synthetic Chemistry, 2016, 24(3): 263-265.
2016, Vol. 24 
