手性磷酸催化的色胺的级联 Michael 加成-环化反应构建吡咯并吲哚啉的对映选择性。
Enantioselective construction of pyrroloindolines via chiral phosphoric acid catalyzed cascade Michael addition-cyclization of tryptamines.
机构信息
State Key Laboratory of Organometallic Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 345 Lingling Lu, Shanghai 200032, China.
出版信息
Org Lett. 2012 Sep 7;14(17):4588-90. doi: 10.1021/ol302043s. Epub 2012 Aug 28.
PMID:22928846
Abstract
Enantioselective construction of pyrroloindolines via chiral phosphoric acid catalyzed cascade Michael addition-cyclization of tryptamines has been realized. With 5 mol % of chiral phosphoric acid, enantioenriched pyrroloindoline derivatives were obtained in good yields and enantioselectivity (up to 95% yield and 83% ee) from readily available tryptamines and enones.
摘要
通过手性磷酸催化的色胺的级联迈克尔加成-环化反应，实现了吡咯并吲哚啉的对映选择性构建。在手性磷酸用量为 5mol%的条件下，从易得的色胺和烯酮出发，以良好的收率和对映选择性（高达 95%的收率和 83%的 ee）得到了富集对映体的吡咯并吲哚啉衍生物。
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