专利号:US-6143887-A 优先权日:1998-05-14 标题:Process for the stereoselective synthesis of 16-substituted-4-aza-androstanones 发明人:GRATALE DOMINICK F; TOLMAN RICHARD L; SAHOO SOUMYA P 权利人:MERCK & CO INC 摘要:The novel process of the present invention involves the stereoselective synthesis of certain 16β-substituted 4-aza-5α-androstan-3-ones and the useful intermediates obtained therein.
专利号:US-6159673-A 优先权日:1996-07-17 标 题:Oxonol compound, light-sensitive material and process for the synthesis of oxonol compound 发明人:NISHIGAKI JUNJI; DEGUCHI YASUAKI 权利人:FUJI PHOTO FILM CO LTD 摘要:An oxonol compound is represented by the following formula (I): in which Z is an atomic group that forms a cyclic amide ring; each of W1 and W2 independently is an atomic group that forms an acidic nucleus ring; and M is a cation. Other oxonol compounds, a light-sensitive material containing an oxonol compound and a process for the synthesis of an oxonol compound are also disclosed.
专利号:US-4266058-A 优先权日:1979-07-04 标 题:Synthesis of 2-isopropylamino-pyrimidine 发明人:DEMOSTHENE CLAUDE G; ASPISI CHRISTIAN R 权利人:SOC D ETUDES PROD CHIMIQUE 摘要:The present invention provides a process for the synthesis of 2-isopropylamino-pyrimidine by aminolysis of 2-methylsulphonyl-pyrimidine using isopropylamine. The aminolysis is effected, according to the present invention, by refluxing isopropylamine and 2-methylsulphonyl-pyrimidine in the absence of a solvent. Using this technique, the 2-isopropylamino-pyrimidine has been obtained in a substantially quantitative yield.
专利号:EP-1473330-B1 优先权日:1996-07-17 标题:Process for the synthesis of oxonol compound 发明人:NISHIGAKI JUNJI; DEGUCHI YASUAKI 权利人:FUJI PHOTO FILM CO LTD 摘要:An oxonol compound is represented by the following formula (I): in which each of Z, W<1> and W<2> independently is an atomic group that forms a heterocyclic ring; and M is a cation. A process for the synthesis of an oxonol compound is disclosed.
专利号:US-2009099218-A1 优先权日:2007-09-17 标题 :Synthesis of novel tubulin polymerization inhibitors: benzoylphenylurea (bpu) sulfur analogs 发明人:KHAN SAEED R; HALLUR GURULINGAPPA; HIDALGO MANUEL; JIMENO ANTONIO 权利人:KHAN SAEED R; HALLUR GURULINGAPPA; HIDALGO MANUEL; JIMENO ANTONIO 摘要:This invention provides a series of BPU analogues; their synthesis and evaluated biological activity. BPU sulfur analogues were found to possess up to 20 fold increased potency, when compared to compound 1, in various cancerous cell lines.
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.