| 摘要 |
Cpds of formula (I): (where Q is NR2R3;R1 is H or 1-3C alkyl, R2 and R3 are H, 1-6C alkyl, 2-6C hydroxyalkyl or 7-9C aralkyl, or NR2R3 is 5- to 7- membered polymethyleneimino or morpholino, both opt. substd by lower alkyl and contg. =10C; A is 1-3C alkylene, rings B and C are opt substd by F,Cl,Br,CF3,NO2,1-6C alkyl or alkoxy) and their 5-oxides and acid addn salts are CNS depressants. They may be prepd. by reacting a reactive ester of (I;Q=OH) with R2R3NH or its alkali metal deriv; reacting a 2-X-3-R1-5-Ph-3H-1,4-benzodiazepine with R2R3NACONHNH2 (where X=SH lower alkoxy or alkylthio (opt. activated by a substd) or opt. substd amino); hydrolysis of (I;Q=R2R3'N) (where R3'=acyl) to give (I;Q=R2HN); reaction of (I;Q=phthalimido) with N2H4 and/or strong acid to give (I;Q=NH2); redn of (I;Q=N3) to give (I;Q=NH2); or reaction of (IfQ=R2HN) with a 1-6C satd aliphatic oxo cpd and reducing the product. |
