Title:A Novel Practical Synthesis of Pazopanib: An Anticancer Drug
VOLUME: 9 ISSUE: 4
Author(s): YiCheng Mei, BaoWei Yang, Wei Chen, DanDan Huang, Ying Li, Xin Deng, BaoMing Liu, JingJie Wang, Hai Qian and WenLong Huang
Affiliation:Center of Drug Discovery, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing, Jiangsu 210009, P.R. China.
Keywords:Anticancer drug, pazopanib, regioselective methylation, synthesis, trimethyl orthoformate, vasculature, dichloropyrimidine, chloride, methylene
Abstract:This paper reports a novel approach to synthesize pazopanib. In our synthetic route, the potently mutagenic alkylating agents such as dimethyl sulfate and methyl iodide are avoided. A novel regioselective methylation of the 2- position of 3-methyl-6-nitro-1H-indazole was reported. This novel route is one step shorter than the previously reported route.
