Highly Enantioselective Fluorination of Unprotected 3‑Substituted Oxindoles: One-Step Synthesis of BMS 204352 (MaxiPost)
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The catalytic enantioselective fluorination of N–H-free 3-substituted oxindoles was accomplished by a Sc(III)/N,N′-dioxide complex. Under mild reaction conditions, a series of 3-aryl- and 3-alkyl-3-fluoro-2-oxindoles were obtained in excellent yields (up to 98%) and enantioselectivities (up to 99% ee) by using N-fluorobisbenzenesulfonimide (NFSI) as the fluorination agent. MaxiPost was synthesized efficiently in 81% yield with 96% ee.
创建时间：
2012-10-19
