An expedient, regioselective synthesis of novel 2-alkylamino- and 2-alkylthiothiazolo[5,4-e]- and -[4,5-g]indazoles and their anticancer potential

作者：Chakrabarty Manas^*; Kundu Taraknath; Arima Shiho; Harigaya Yoshihiro

来源：Tetrahedron, 2008, 64(28): 6711-6723.

DOI：10.1016/j.tet.2008.05.009

• thiazolo[5,4-e]- and -[4,5-g]indazoles
• anticancer
• regioselective synthesis
• thioureidoindazoles
• indazolyl dithiocarbamates
• bromine in acetic acid

Several novel 2-alkylamino- and 2-alkylthiothiazolo[5,4-e]- and -[4,5-g]indazoles and their 6-alkyl and 8-alkyl derivatives have been synthesised in high overall yields starting from 5-nitro and 6-nitro-indazoles in a three-step route involving the regioselective cyclisation of thioureidoindazoles and indazolyl dithiocarbamates as the key steps. Some assorted thiazoloindazoles have been screened for anticancer properties, which demonstrated the anticancer potential of at least one product, justifying its further follow-up.

• 出版日期2008-7-7