通过金催化的N-（邻炔基芳基）-N-乙烯基磺酰胺的区域选择性环异构化反应简便合成1-苯并氮杂卓衍生物。
The facile synthesis of 1-benzoazepine derivatives via gold-catalyzed regioselective cycloisomerization reactions of N-(o-alkynylaryl)-N-vinyl sulfonamides.
作者信息
Undeela Sridhar, Ravikumar Gurram, Nanubolu Jagadeesh Babu, Singarapu Kiran Kumar, Menon Rajeev S
机构信息
Medicinal Chemistry and Pharmacology Division, CSIR-Indian Institute of Chemical Technology, Hyderabad, 500 007, India.
出版信息
Chem Commun (Camb). 2016 Apr 4;52(26):4824-7. doi: 10.1039/c6cc01061j. Epub 2016 Mar 11.
Gold-catalyzed, regioselective cycloisomerization of N-(o-alkynylaryl)-N-vinyl sulfonamides afforded high yields of 2-sulfonylmethyl-1-benzoazepine derivatives. This 7-endo-dig selective cyclization proceeds via the incorporation of an exocyclic double bond by a labile 1-benzoazepine intermediate. The cyclization substrates were assembled in two steps from readily available materials using Sonogashira coupling and a Cs2CO3-mediated formal vinylic substitution.
金催化的N-（邻炔基芳基）-N-乙烯基磺酰胺的区域选择性环异构化反应能高产率地得到2-磺酰基甲基-1-苯并氮杂卓衍生物。这种7-内型-双烯选择性环化反应通过一个不稳定的1-苯并氮杂卓中间体引入环外双键来进行。环化反应底物由容易获得的原料通过Sonogashira偶联反应和碳酸铯介导的形式上的乙烯基取代反应分两步组装而成。
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