发明名称 PROCESS FOR PREPARING 3-(4-AMINOETHOXYBENZOYL)BENZO(B)THIOPHENES
摘要 <p>Compds. of the formula (I) [R = H; R1 = COC6H4O(CH2)2NR2R3; R2 = R3 =alkyl; R2R3 = (CH2)4-6, (CH2)2OC(CH2)2, etc. and their acid addn. salts were prepd. by Friedel-Crafts acylation of (I) [R = Ac, Bz, MeSO2; R1 = H followed by hydrolysis of the ester gps. Thus, HSC6H4OMe-3 was treated with BrCH2COC6H4OMe-4 to give 3- MeOC6H4SCH2COC6H4OMe-4, which was cyclized with polyphosphoric acid to give (I) [R = Me, R1 = H . Penethylation of the latter followed by esterification with MeSO2Cl gave (I) [R = MeSO2, R1= H; II . Friedel- Crafts acylation of 4g(II) with 4-Me2N(CH2)2OC6H4COCl gave 6.2g (I) [R1 = MeSO2, R1 = COC6H4O (CH2)NMe-4, III . Hydrolysis ofd III gave I [R = H . (I) are used for treating the hormone-dependent tumors.</p>
申请公布号 KR850001882(B1) 申请公布日期 1985.12.28
申请号 KR19820001470 申请日期 1982.04.02
申请人 ELI LILLY AND CO. 发明人 JONES, CHARLES DAVID;GOETTEL, MARY ELIZABETH
分类号 C07D333/52;C07D333/56;(IPC1-7):C07D333/52 主分类号 C07D333/52
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