通过腈与给体-受体环丙烷的环加成反应合成 5-氮吲哚。
Synthesis of 5-azaindoles via a cycloaddition reaction between nitriles and donor-acceptor cyclopropanes.
机构信息
Department of Chemistry, The University of Western Ontario, London, Ontario, N6A 5B7, Canada.
出版信息
Org Lett. 2010 Jul 16;12(14):3168-71. doi: 10.1021/ol101078z.
PMID:20550103
Abstract
A new method for the synthesis of 5-azaindole derivatives is reported. A [3+2] dipolar cycloaddition between nitriles and a 3,4-cyclopropanopiperidine followed by SeO(2) oxidation affords the target compounds in moderate to excellent yields. The divergent nature and cost effectiveness of this method makes it very suitable for combinatorial applications in the pharmaceutical industry.
摘要
报道了一种合成 5-氮吲哚衍生物的新方法。腈与 3,4-环丙烷哌啶之间的[3+2]偶极环加成，随后用 SeO(2)氧化，以中等至优异的收率得到目标化合物。该方法具有多样性和成本效益，非常适合制药工业中的组合应用。
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