利用三氮唑的4+3环化反应合成1,4-氧氮杂█  

Synthesis of 4,5-Dihydro-1,4-oxazepines via 4+3 Cyclization of Triazoles

作　　者：郑坚萍 修世东 Zheng Jianping;Xiu Shidong(Quality Department,Hangzhou MSD Pharmaceutical Company Limited,Hangzhou 310018;Department of Chemistry,Zhejiang Sci-Tech University,Hangzhou 310018,China)

机构地区：[1]杭州默沙东制药有限公司质量部,浙江杭州310018 [2]浙江理工大学化学系,浙江杭州310018

出　　处：《广东化工》2021年第6期16-17,共2页Guangdong Chemical Industry

摘　　要：报道了一种合成1,4-氧氮杂?的新方法。利用1-磺酰基-1,2,3-三氮唑与α,β-不饱和醛为原料,以Rh2(Oct)4为催化剂,1,2-DCE为溶剂,在氮气氛下回流,以中等产率得到非苯并氧氮杂?衍生物。该反应经α-亚胺基铑卡宾的4+3成环历程,设计新颖,操作简单。A new method for synthesis of 4,5-dihydro-1,4-oxazepines is reported. Using readily available 1-sulfonyl-1,2,3-triazoles and α,β-unsaturated aldehydes as starting materials, 1,4-oxazepines were synthesized conveniently in moderate yields in the presence of Rh2(Oct)4. Moreover, this transformation manifests the potential utility of 1-sulfonyl-1,2,3-triazole as precursor of aza-1,3-dipole in formal 4+3 cyclization.

关 键 词：氧氮杂█ 三氮唑 α-亚胺基卡宾 4+3环化 

分 类 号：O626.3[理学—有机化学]