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DIBENZO(B,E)OXEPIN DERIVATIVE AND ANTIALLERGIC AGENT CONTAINING SAID DERIVATIVE AS ACTIVE COMPONENT

机译:包含所述衍生物的双苯并(B,E)氧杂环丁烷衍生物和抗痛剂为有效成分

摘要

NEW MATERIAL:The dibenzo[b,e]oxepin derivative of formula I {R1 is cyano, 5-tetrazolyl, carbamoyl or -CO2R3 [R3 is H, alkyl or 1-(ethoxycarbonyloxy)ethyl]; R2 is 4-alkylpiperazino, 3-quinuclidylamino or -X-(CH2)n-NR4R5 (X is -NH, S or O; R4 and R5 are alkyl; n is 2 or 3)}, its acid addition salt or metallic salt. EXAMPLE:11-(4-Methylpiperazino)-6,11-dihydrodibenzo[ b,e ]oxepin-2-carboxylic acid ethyl ester. USE:It has antiallergic activity and is useful as a remedy for asthma, etc. as an antiallergic agent. It is administered preferably by oral administration or injection. PREPARATION:The compound of formula I is prepared from the o-halomethylbenzoic acid of formula II and the alkali metal salt of formula III via various reaction steps.
机译:新材料:式I的二苯并[b,e]氧杂环丁烷衍生物[R1是氰基,5-四唑基,氨基甲酰基或-CO2R3 [R3是H,烷基或1-(乙氧基羰氧基)乙基]; R 2为4-烷基哌嗪子基,3-喹啉基氨基或-X-(CH 2)n -NR 4 R 5(X为-NH,S或O; R 4和R 5为烷基; n为2或3)},其酸加成盐或金属盐。实施例:11-(4-甲基哌嗪子基)-6,11-二氢二苯并[b,e]氧杂环丁-2-羧酸乙酯。用途:具有抗过敏作用,可用作哮喘等的抗过敏药。优选通过口服或注射给药。制备:式I化合物是通过各种反应步骤由式II的邻卤甲基苯甲酸和式III的碱金属盐制备的。

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