稠合喹喔啉 - 苯并二氮杂卓和双苯并二氮杂卓的两步合成法。
Two step syntheses of fused quinoxaline-benzodiazepines and bis-benzodiazepines.
作者信息
Xu Zhigang, Dietrich Justin, Shaw Arthur Y, Hulme Christopher
机构信息
College of Pharmacy, Department of Pharmacology and Toxicology, Division of Medicinal Chemistry, BIO5 Institute, Southwest Comprehensive Center for Drug Discovery and Development, University of Arizona, AZ 85721.
出版信息
Tetrahedron Lett. 2010 Aug 25;51(34):4566-4569. doi: 10.1016/j.tetlet.2010.06.116.
Abstract
A two-step solution phase synthesis employing a double UDC (Ugi/Deprotect/Cyclize) strategy has been utilized to obtain fused 6,7,6,6-quinoxalinone-benzodiazepines and 6,7,7,6-bis-benzodiazepines. Optimization of the methodology to produce these tetracyclic scaffolds was enabled by microwave irradiation, incorporation of trifluoroethanol as solvent, and the use of the convertible isocyanide, 4-tert-butyl cyclohexen-1-yl isocyanide.
摘要
采用双UDC（Ugi/脱保护/环化）策略的两步溶液相合成法已被用于获得稠合的6,7,6,6-喹喔啉酮-苯并二氮杂卓和6,7,7,6-双苯并二氮杂卓。通过微波辐射、加入三氟乙醇作为溶剂以及使用可转化的异氰化物4-叔丁基环己烯-1-基异氰化物，实现了生产这些四环骨架方法的优化。
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