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参考文献:N-Substituted Nonaryl-Heterocyclic Nmda/nr2B Antagonists
标题:N-Substituted Nonaryl-Heterocyclic Nmda/nr2B Antagonists
摘要:由化学式(i)表示的化合物及其药学上可接受的盐,可作为nmda Nr2B拮抗剂,用于缓解疼痛.
专利信息
专利号:US-5304647-A
优先权日:1988-02-09
标题:Method of preparation of halogenated diazines
发明人:STREKOWSKI LUCJAN; MOKROSZ MARIA; HARDEN DONALD B
权利人:UNIV GEORGIA STATE
摘要:A method of preparation of substituted halogenodiazines which are useful as intermediates in the synthesis of novel unfused heterobicyclic compounds, and the products thereof. The reaction consists of the addition of an organolithium reagent with subsequent dehydrogenation of the addition product. The reaction takes place in one reaction vessel, without isolation of the substituted halogenodihydrodiazine intermediate. The reactions proceed at moderate temperature and in a short amount of time, which decreases the probability of side reactions and increases yield. Furthermore, the workup step is conducted under two-phase conditions to prevent hydrolysis of the substituted halogenodiazine to a substituted hydroxydiazine. The method is easy, efficient and results in a high yield of product. The substituted halogenodiazines are used as intermediates in the synthesis of unfused heterobicyclic compounds containing an aromatic moiety, diazine, and another aromatic moiety, such as thiophene, benzene, or naphthalene, which have biological activity.
专利号:US-4963676-A
优先权日:1988-02-09
标题 :Di-substituted phthalazines
发明人:STREKOWSKI LUCJAN; MOKROSZ MARIA; HARDEN DONALD B
权利人:UNIV GEORGIA STATE
摘要:A method of preparation of substituted halogenodiazines which are useful as intermediates in the synthesis of novel unfused heterobicyclic compounds, and the products thereof. The reaction consists of the addition of an organolithium reagent with subsequent dehydrogenation of the addition product. The reaction takes place in one reaction vessel, without isolation of the substituted halogenodihydrodiazine intermediate. The reactions proceed at moderate temperature and in a short amount of time, which decreases the probability of side reactions and increases yield. Furthermore, the workup step is conducted under two-phase conditions to prevent hydrolysis of the substituted halogenodiazine to a substituted hydroxydiazine. The method is easy, efficient and results in a high yield of product. The substituted halogenodiazines are used as intermediates in the synthesis of novel unfused heterobicyclic compounds containing an aromatic moiety, diazine, and another aromatic moiety, such as thiophene, benzene, or naphthalene, which have biological activity.