3-溴吲哚促进的烯醇化物芳基化反应能够形成β-咔啉。
Catalytic Enolate Arylation with 3-Bromoindoles Allows the Formation of β-Carbolines.
机构信息
Department of Chemistry, University of Oxford, Chemistry Research Laboratory , Mansfield Road, Oxford OX1 3TA, U.K.
AstraZeneca, Pharmaceutical Sciences , Silk Road Business Park, Macclesfield SK10 2NA, U.K.
出版信息
J Org Chem. 2017 Apr 21;82(8):4435-4443. doi: 10.1021/acs.joc.7b00299. Epub 2017 Mar 31.
PMID:28362489
Abstract
Synthesis of substituted β-carbolines was accomplished by utilizing the catalytic enolate arylation reaction of ketones in conjunction with several 3-bromoindole derivatives. Quenching of the arylation reaction in situ with an electrophile allowed ready incorporation of functionality at the carboline C-4 position in an efficient one-pot protocol.
摘要
取代β-咔啉的合成立足于酮的催化烯醇芳基化反应，并结合几种 3-溴吲哚衍生物。芳基化反应在原位用亲电试剂淬灭，允许在有效的一锅法方案中在咔啉 C-4 位置容易地引入官能团。
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