Chinese Journal of Organic Chemistry, Journal Year: 2021, Volume and Issue: 41(8), P. 3256 - 3256
Published: Jan. 1, 2021
Direct conversion of ortho-aminobenzacetamides and ortho-aminobenzacetates to the corresponding 1H-indazole-3-carboxylic acid derivatives under action diazotization reagents was reported.This method features operational simplicity, mild reaction conditions, rapid rates, high yields, wide substrate scope, offering an efficient concise route synthesis derivatives.The drugs granisetron lonidamine were synthesized successfully using this protocol with 46% 60% total respectively.Preliminary mechanistic study suggests that diazonium salt is a key intermediate.
Language: Английский