Synthesis of Succinimide-Linked Indazol-3-ols Derived from Maleimides under Rh(III) Catalysis
Ju Young Kang1, Suho Kim1, Junghyea Moon1
1School of Pharmacy, Sungkyunkwan University, 2066 Seobu-ro, Jangan-gu, Jangan-gu, Suwon, Gyeonggi 16419, Republic of Korea.
Abstract:
The structural modification of N-aryl indazolols as tautomers of N-aryl indazolones has been established as a hot topic in pharmaceutics and medicinal chemistry. We herein disclose the rhodium(III)-catalyzed 1,4-addition reaction of maleimides with N-aryl indazol-3-ols, which provides the succinimide-bearing indazol-3-ol scaffolds with complete regioselectivity and a good functional group tolerance. Notably, the versatility of this protocol is demonstrated by the use of drug-molecule-linked and fluorescence-probe-linked maleimides.
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