Synthesis of tricyclic 4-chloro-pyrimido[4,5-b][1,4]benzodiazepines |
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Authors: | Yang Jianxin Che Xin Dang Qun Wei Zhonglin Gao Shu Bai Xu |
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Institution: | The Center for Combinatorial Chemistry and Drug Discovery, Jilin University, 75 Jinlai Street, Changchun, Jilin 130012, P. R. China. |
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Abstract: | reaction: see text] A novel methodology was developed for the efficient synthesis of 4-chloro-pyrimido4,5-b]1,4]benzodiazepines. The key is the intramolecular Friedel-Crafts cyclization of 5-amino-4-(N-substituted)anilino-6-chloropyrimidine with either a carboxylic acid or its derivatives to construct the 4-chloro-pyrimido4,5-b]1,4]benzodiazepine core. Subsequent nucleophilic substitution allows the introduction of one more diversity point in the target molecules. This strategy provides an efficient method to access a library of compounds based on privileged substructures that are of great interest in drug discovery. |
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