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【结 构 式】 
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【药物名称】Cloturin, VUFB-15686 【化学名称】N-(2-Chloroethyl)thiocarbamic acid 6-purinyl ester 【CA登记号】104789-46-0, 116861-52-0 ([35S]-labeled) 【 分 子 式 】C8H8ClN5OS 【 分 子 量 】257.70286 |
【开发单位】Res. Inst. Pharmacy Biochemistry (VUFB) (Originator), SPOFA (Originator) 【药理作用】ONCOLYTIC DRUGS, Antimetabolites |
合成路线1
The compound can be prepared by reacting mercaptopurine (I) with 2-chloroethylisocyanate (II) in an inert medium at a temperature from 0-50 C, preferably in the presence of an alkaline agent. Suitable inert media for the reaction are dimethylformamide, dimethylsulfoxide, phosphoric acid, hexamethyltriamide or tetramethylurea. Alkaline agents, preferably tertiary organic amines, accelerate the reaction and make the yield of the desired product higher.
| 【1】 Cerny, A.; Krepelka, J.I.; Melka, M.; Molko, M.; Pokorná, S.; Reichová, R.; Kejhová, I.; Beitová, M.; Grimová, J. (SPOFA - United Pharmaceutical Works); 6-Purinyl N-(2-chloroethyl)carbamate and thiocarbamate, a process for their preparation and use thereof. CS 249576. EP 0186454; JP 1986186382; US 4720497 . |
| 【2】 Melka, M.; Krepelka, J.; Miko, M.; CLOTURIN. Drugs Fut 1990, 15, 4, 337. |