参考标题:Synthesis Of 1,4-Benzodiazepin-3-Ones And 1,5-Benzodiazocin-4-Ones By Addition Of Grignard Reagents To Derivatives Of O-Aminobenzonitrile 作者:Birgitta Pettersson,Anna Rydbeck,Jan Bergman 摘要:Addition Of Organometallics To N-(α-Haloacyl)-O-Aminobenzonitrile Resulted In The Formation Of 2,5-Disubstituted 1,4-Benzodiazepin-3-Ones, Whereas N-(β-Haloacyl)-O-Aminobenzonitrile Gave 2,6-Disubstituted 1,5-Benzodiazocin-4-Ones Under Similar Conditions. Initial Cylization Of N-(β-Haloacyl)-O-Aminobenzonitrile To Obtain The Corresponding Lactam (E.G.α,α-Dimethyl-N-(2-Cyanophenyl)-β-Lactam) Increased The Yield Of 1,5-Benzodiazocin-4-Ones Significantly. Somewhat Surprisingly, Addition Of Lithium Reagents To N-(β-Haloacyl)-O-Aminobenzonitrile Gave 4,4-Disubstituted Quinazolines Viagrob Fragmentation.