Rh(III)-Catalyzed C-H Functionalization of Indolines with Readily Accessible Amidating Reagent: Synthesis and
Mijin Jeon1, Neeraj Kumar Mishra1, Umasankar De1
1School of Pharmacy, Sungkyunkwan University , Suwon 16419, Republic of Korea.
Abstract:
The rhodium(III)-catalyzed direct C-H functionalization of various indolines with 1,4,2-dioxazol-5-ones as new amidating agents is described. This transformation provides efficient preparation of C7-amidated indolines known to display potent anticancer activity. The synthetic compounds were evaluated for in vitro anticancer activity against human prostate adenocarcinoma cells (LNCaP), human endometrial adenocarcinoma cells (Ishikawa), and human ovarian carcinoma cells (SKOV3). Compound 4f was found to be highly cytotoxic, with activity competitive with that of anticancer agent doxorubicin.
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