Novel Synthesis of Arylethynyl-Heterocyles
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چکیده
The tosyl group has been one of the most commonly used groups to protect, activate and chelate indoles for lithiation at position 2. In the course of one of our synthetic programs, 1-tosyl-2-(pmethoxyphenylacetyl)indole (1a) was prepared in excellent yields starting from N-tosylindole by 2lithiation, transformation of the resulting 2-lithio derivative into the 2-trimethylstannylindole derivative, and finally, Pd(0) catalyzed cross-coupling with pmethoxyphenylacetyl chloride (Scheme 1).
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تاریخ انتشار 2013