CAS: 698-80-6; 4-(Chloromethyl)-1,2-Difluorobenzene

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CAS号542-88-1 二氯甲基醚 | CAS号367-11-3 邻二氟苯 | CAS号658-93-5 3,4-二氟苯乙酸 | CAS号658-99-1 3,4-二氟苯乙腈

3,4-二氟苯甲醇置于氯化亚砜体系中,用 二氯甲烷 作为反应溶剂,化学反应生成 3,4-二氟氯苄
参考文献:1H-咪唑-2-羧酸衍生物的结构引导优化,可提供有效的 Vim 型金属-β-内酰胺酶抑制剂
标题:1H-咪唑-2-羧酸衍生物的结构引导优化,可提供有效的 Vim 型金属-β-内酰胺酶抑制剂
摘要:细菌病原体中金属-β-内酰胺酶 (Mbl) 的产生是对"最后手段"碳青霉烯类抗生素产生耐药性的重要原因.仍然需要开发有效的 Mbl 抑制剂来逆转革兰氏阴性菌对碳青霉烯类的耐药性.我们在此报告了 1 H的 X 射线结构引导优化-咪唑-2-羧酸(ica)衍生物,通过考虑如何与活性位点柔性环结合并提高对革兰氏阴性细菌的渗透.构效关系研究揭示了在 Ica 1 位适当的取代基对于实现对 B1 类 Mbls,特别是 Verona Integron 编码的 Mbls (Vims) 的有效抑制的重要性,主要是通过与灵活的活性位点环的巧妙相互作用,如观测到的那样晶体学分析.在测试的 Ica 抑制剂中,55种与美罗培南对工程大肠杆菌菌株甚至难治的临床分离的铜绿假单胞菌具有最强的协同抗菌活性生产 Vim-2 Mbl.处理后细菌细胞的形态和内部结构变化进一步证明55穿过外膜并逆转美罗培南的活性.此外,55在体内
DOI:10.1016/j.Ejmech.2021.113965

专利信息

专利号:US-4536599-A
优先权日:1978-08-22
标题:Synthesis of amine derivatives
发明人：MASUKO FUJIO; KATSURA TADASHI
权利人:SUMITOMO CHEMICAL CO
摘要:An amine of the formula, ##STR1## wherein R 1 , R 2 , R 3 , R 4 and R 5 are each hydrogen, alkyl or the like and n is 1, 2 or 3, including α-phenyl-β-(p-tolyl)-ethylamine, which is useful as an optically resolving agent, an intermediate of medicines and the like, is effectively produced by a novel process comprising hydrolysis of the corresponding nitrile of the formula, ##STR2## wherein R 1 , R 2 , R 3 , R 4 , R 5 and n are the same as above, followed by alkali-decomposition of the resulting amide of the formula, ##STR3## wherein R 1 , R 2 , R 3 , R 4 , R 5 and n are the same as above. An amide including the above one is effectively produced by hydrolysis of the corresponding nitrile in the presence of a base and hydrogen peroxide using an organic quaternary ammonium salt and/or a tertiary amine as a catalyst.

专利号:US-7396846-B2
优先权日:2002-04-09
标题:Growth hormone secretagogues
发明人：EVERS BRITTA; GERD RUEHTER; MARTIN DE LA NAVA EVA MARIA; TEBBE MARK JOSEPH
权利人:LILLY CO ELI
摘要:This invention relates to novel compounds which are useful in the modulation of endogenous growth hormone levels in a mammal. The invention further relates to novel intermediates for use in the synthesis of said compounds, as well as novel processes employed in these syntheses. Also included are methods of treating a mammal which include the administration of said compounds.

专利号:EP-0008532-A1
优先权日:1978-08-22
标 题 :Synthesis of amines

专利号:EP-0008532-B1
优先权日:1978-08-22
标 题 :Synthesis of amines

专利号:EP-0040896-A2
优先权日:1978-08-22
标 题 :Synthesis of amides

专利号:WO-2016091228-A1
优先权日:2014-12-11
标题 :Substituted phenyltetrazole, its use and pharmaceutical preparation containing it
发明人：ROH JAROSLAV; NEMECEK JAN; HRABALEK ALEXANDR; KLIMESOVA VERA; KARABANOVICH GALINA; PAVEK PETR; SYCHRA PAVEL
权利人:UNIV KARLOVA
摘要:A nitro group-substituted phenyltetrazole of general formula (I) wherein R is selected from the group consisting of: H, C 1 -C 11 alkyl, phenyl- or phenyl- substituted in positions 2, 3, 4 or 5 by one or more electron-acceptor groups and/or by one or more electron-donor groups. These compounds can be prepared by easy synthesis and have significant activity against mycobacteria including their multidrug resistant strains. The invention provides also a pharmaceutical preparation having nitro group-substituted phenyltetrazole of formula (I) as the active ingredient, as well as the use of this nitro group-substituted phenyltetrazole as antituberculosis drug.