| 摘要 |
NEW MATERIAL:A compound of formula I (R<1> is residue of carboxylic acid; R<2> is lower alkyl; R<3> is H, lower alkyl). EXAMPLE:5,10,11,11a-Tetrahydro-9- ( 3-carboxypropanoyloxy ) -11-hydroxy-8-methyl-5-oxo-1H-pyrolo-[2,1-c][1,4]-benzoazepine-2-acryl amide. USE:Antitumor agent: it is soluble in water and has decreased toxicity and local impairment. PREPARATION:For example, a compound of formula II or its lower alkyl ether in the 11-position such as 5,10,11,11a-tetrahydro-9-hydroxy-11-methoxy-8-methyl- 5-oxo-1H-pyrolo-[2,1-c][1,4]-benzodiazepine-2-acrylamide is allowed to react with a cyclic acid anhydride such as succinic anhydride, preferably in the presence of a base or acid catalyst at room temperature to 100 deg.C.
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