Abstract

The manuscript describes an efficient, atom economical synthesis of pyrimido[4,5-b][1,4]benzodiazepin-4-ones by relatively unexplored 7-endo-trig Pictet–Spengler type cyclisations. The synthetic methdodlogy involves the synthesis of different variants of 5-arylidene-amino-3H-pyrimidines and their p-toluene sulfonic acid mediated 7-endo-trig Pictet–Spengler type cyclisations to afford biologically relavent functionalized benzodiazepine condensed pyrimidinones such as pyrimido[4,5-b][1,4]benzodiazepines in good to excellent yields (82–94%).

中文翻译：

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5-亚烷基/亚芳基-氨基-3H-嘧啶-4-酮的7-内-trig Pictet-Spengler型环化：嘧啶基[4,5-b] [1,4]苯并二氮杂卓的高效非对映选择性合成

摘要

该手稿描述了通过相对未开发的7-内-trig Pictet-Spengler型环化方法高效，原子经济地合成嘧啶并[4,5-b] [1,4]苯并二氮杂-4-酮的方法。合成方法学涉及5-亚芳基-氨基-3H-嘧啶的不同变异体及其对甲苯磺酸介导的7-内-trig Pictet-Spengler型环化反应的合成，以提供具有生物学相关性的功能化苯并二氮杂稠合嘧啶酮类化合物，如嘧啶基[4]。 ，5-b] [1,4]苯二氮杂类化合物的收率好至极好（82-94％）。