摘要
3-甲基-6-硝基-2H-吲唑(3)经甲基化、还原、单甲基化后,与2,4-二氯嘧啶缩合制得2,3-二甲基-N-(2-氯嘧啶-4-基)-N-甲基-2H-吲唑-6-胺,再与2-甲基-5-氨基苯磺酰胺经缩合、成盐酸盐制得抗肿瘤药盐酸帕唑帕尼,总收率约为37%。
Pazopanib hydrochloride was synthesized from 3-methyl-6-nitro-2H-indazole （3） by methylation, reduction, monomethylation and coupled with 2,4-dichloropyrimidine to give 2,3-dimethyl-N-（2-chloropyrimidin-4-yl）- N-methyl-2H-indazol-6-amine, which was condensed with 2-methyl-5-aminobenzene sulfonamide and then salt formation with an overall yield of about 37%.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2012年第8期644-646,共3页
Chinese Journal of Pharmaceuticals
基金
国家“重大新药创制”科技重大专项(2009ZX09301-007)
关键词
盐酸帕唑帕尼
抗肿瘤药
合成
pazopanib hydrochloride
antitumor agent
synthesis
