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.
Keywords: Anticancer drug, pazopanib, regioselective methylation, synthesis, trimethyl orthoformate, vasculature, dichloropyrimidine, chloride, methylene
Letters in Organic Chemistry
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, WenLong Huang
Affiliation:
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.
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YiCheng Mei, BaoWei Yang, Wei Chen, DanDan Huang, Ying Li, Xin Deng, BaoMing Liu, JingJie Wang, Hai Qian, WenLong Huang , A Novel Practical Synthesis of Pazopanib: An Anticancer Drug, Letters in Organic Chemistry 2012; 9 (4) . https://dx.doi.org/10.2174/157017812800233714
DOI https://dx.doi.org/10.2174/157017812800233714 |
Print ISSN 1570-1786 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6255 |
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