摘要
Benzodiazepine and benzothiazepine derivatives have been well known as therapeutically important compounds. Four new tricyclic heterocyclic compounds, 3a, 4, 5, 11-tetrahydro-3H-l,2, 4-triazalo [4, 3-d] [1, 5] benzothiazepines (3), 3a, 4, 5, 11-tetrahydro-3H,6H-1, 2, 4-triazolo[4, 3-d] [1, 5]benzodiazepine (4), 3a, 4, 5, 11-tetrahydro-1, 2, 4-oxadiazolo [4, 5-d] [1, 5]benzothiazepines (5, 6) and 3a,4, 5, 11-tetrahydro-6H-1, 2, 4-oxadiazolo[4, 5-d] [1, 5] benzodiazepines (7, 8), have been synthesized by 1, 3-dipolar cycloaddition reactions of 2, 3-dihydro-1, 5-benzothiazepines and 2, 3-dihydro-1H-1, 5-benzodiazepine with benzonitrile N-phenylimine and benzonitrile oxides, receptively. The conformations of some cycloadducts and cycloaddition mechanism are described.
Benzodiazepine and benzothiazepine derivatives have been well known as therapeutically important compounds. Four new tricyclic heterocyclic compounds, 3a, 4, 5, 11-tetrahydro-3H-l,2, 4-triazalo [4, 3-d] [1, 5] benzothiazepines (3), 3a, 4, 5, 11-tetrahydro-3H,6H-1, 2, 4-triazolo[4, 3-d] [1, 5]benzodiazepine (4), 3a, 4, 5, 11-tetrahydro-1, 2, 4-oxadiazolo [4, 5-d] [1, 5]benzothiazepines (5, 6) and 3a,4, 5, 11-tetrahydro-6H-1, 2, 4-oxadiazolo[4, 5-d] [1, 5] benzodiazepines (7, 8), have been synthesized by 1, 3-dipolar cycloaddition reactions of 2, 3-dihydro-1, 5-benzothiazepines and 2, 3-dihydro-1H-1, 5-benzodiazepine with benzonitrile N-phenylimine and benzonitrile oxides, receptively. The conformations of some cycloadducts and cycloaddition mechanism are described.
基金
Project (No. 29342036) supported by the Natural Science Foundation of China.
