N - boc -3-羟基吡咯烷的区域选择性定向锂化。2-取代4-羟基吡咯烷的合成

Sunose Mihiro, T. Peakman, J. Charmant, T. Gallagher, S. Macdonald
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引用次数: 11

摘要

N-Boc 3-羟基吡咯烷1在C5发生定向碳锂化,而不是像以前报道的那样在C2发生定向碳锂化;得到的稀释中间体6被一系列亲电试剂捕获,得到2-取代的4-羟基吡咯烷7。
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Regioselective directed lithiation of N -Boc-3-hydroxypyrrolidine. Synthesis of 2-substituted 4-hydroxypyrrolidines
N-Boc 3-hydroxypyrrolidine 1 undergoes directed C-lithiation at C5 and not, as previously reported, at C2; the resulting dilithiated intermediate 6 has been trapped by a range of electrophiles to give 2-substituted 4-hydroxypyrrolidines 7.
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