(R)-3-(4-Bromophenoxy)-2-Methylpropane-1,2-Diol置于tris-(Dibenzylideneacetone)Dipalladium(0),2-二叔丁基磷-2-(N,N-二甲氨基)联苯 三正丁胺,Sodium Acetate,Potassium Carbonate,三乙胺,Potassium Hydroxide体系中,用 甲醇,醋酸叔丁酯,乙酸乙酯,Xylene 作为反应溶剂,化学反应 26.83H,反应生成 迪拉马尼 参考文献: Synthetic Intermediate Of Oxazole Compound And Method For Producing The Same[fr] Intermédiaire Synthétique D'Un Composé Oxazole Et Procédé De Production Associé 标题: Synthetic Intermediate Of Oxazole Compound And Method For Producing The Same[fr] Intermédiaire Synthétique D'Un Composé Oxazole Et Procédé De Production Associé 摘要:本发明的目的是提供一种高产率生产噁唑化合物的方法.该目的可以通过由式(11)表示的化合物实现:其中r1是氢原子或较低的烷基基团;r2是在4-位被取代的1-哌啶基团,所述取代基选自(a1A)苯氧基在苯基上取代一个或多个卤素取代的较低烷氧基团,(a1B)苯氧基取代的较低烷基基团在苯基上取代一个或多个卤素取代的较低烷基基团,(a1C)苯基取代的较低烷氧基较低烷基基团在苯基上取代卤素,(a1D)苯基取代的较低烷基基团在苯基上取代一个或多个卤素取代的较低烷氧基团,(a1E)氨基取代的苯基取代一个或多个卤素取代的较低烷氧基团和较低烷基基团,以及(a1F)苯基取代的较低烷氧基团在苯基上取代一个或多个卤素取代的较低烷氧基团;n是1到6之间的整数;x3是有机磺酰氧基团.
专利号:US-11744867-B2 优先权日:2017-02-14 标 题 :Modulation of microbial synthesis of 4-ethylphenol and 4-ethylphenyl sulfate in behavior and disease 发明人:NEEDHAM BRITTANY D; MAZMANIAN SARKIS K; SHARON GIL; FUNABASHI MASANORI; FISCHBACH MICHAEL A; HSIAO ELAINE Y; PATTERSON PAUL H 权利人:CALIFORNIA INST OF TECHN; UNIV CALIFORNIA 摘要:Some embodiments relate to genetically engineered bacterial strains for modulation of levels of the bacterial metabolite 4-ethylphenol (4EP) and its sulfated form, 4-ethylphenyl sulfate (4EPS). In some embodiments, the bacteria reduce or inhibit production of 4EP or 4EPS in the gut of a subject. The bacteria can ameliorate, delay the onset, or reduce the likelihood of one or more symptoms associated with anxiety and/or autism spectrum disorder (ASD) in the subject.
专利号:US-9908876-B2 优先权日:2009-11-05 标 题:Imidazo [1,2-a]pyridine compounds, synthesis thereof, and methods of using same 发明人:MILLER MARVIN J; MORASKI GARRETT C; MARKLEY LOWELL D; DAVIS GEORGE E 权利人:UNIV NOTRE DAME DU LAC 摘要:Embodiments relate to the field of chemistry and biochemistry, and, more specifically, to imidazopyridine compounds, synthesis thereof, and methods of using same. Disclosed herein are various imidazo[1,2-a]pyhdine compounds and methods of using the novel compounds to treat or prevent tuberculosis in a subject or to inhibit fungal growth on plant species. Other embodiments include methods of synthesizing imidazo[1,2-a]pyridine compounds, such as the disclosed imidazo[1,2-a]pyridine compounds.
专利号:US-2023242482-A9 优先权日:2019-07-26 标 题:Discovery, total synthesis, and bioactivity of doscadenamides 发明人:LUESCH HENDRIK; LIANG XIAO; MATTHEW SUSAN; KWAN JASON C; CHEN QI-YIN; PAUL VALERIE J 权利人:UNIV FLORIDA; SMITHSONIAN INST 摘要:The invention is directed towards compounds (e.g., Formulae (I)-(IX)), their mechanism of action, processes to prepare the compounds, methods of activating quorum sensing signaling activity, and methods of treating diseases and disorders using the compounds described herein (e.g., Formulae (I)-(IX)).
专利号:WO-2014161516-A1 优先权日:2013-04-04 标 题 :Oxa- and thia-diazoles useful in the treatment of tuberculosis 发明人:HRABALEK ALEXANDR; ROH JAROSLAV; KARABANOVICH GALINA; KLIMESOVA VERA; NEMECEK JAN; PAVEK PETR 权利人:UNIVERZITA KARLOVA V PRAZE FARMACEUTICKA FAKULTA V HRADCI KRALOVE 摘要:A substituted diazole of genera l formula (1) wherein X is 0 or S; R is selected from the group consisting of: H, NH2-, C 1 -C 11 n alkyl, cyclohexyl-, benzyl-, phenyl-, pyridyl- or phenyl- substituted, in positions 2, 3, 4 or 5, by one or more electron-acceptor groups comprising -N02, -N(a lkyl)3, -CF 3 , CC 13, -CN, -COOH, -COOAlk, -COOAr, -CHO, -COAlk, -COAr, -F, -CI, -Br, -I, and/or electron-donor groups comprising -NH 2 , -N Halkyl, -N(alkyl)2, -OH, -Oalkyl, -Oaryl, -NHCOCH 3 , -NHCOalkyl; -NHCOaryl; -alkyl, -aryl, wherein when R 1 and R 3 is -N0 2 , then R 2 a R 4 is -H, or when R 1 and R 3 is -H, then R 2 and R 4 is -N0 2 . These compounds can be prepared by easy synthesis and have low toxicity and significant activity against mycobacteria including their multiresistant strains. The invention provides also a pharmaceutical preparation having substituted diazole of formula (I) as the active ingredient, as well as the use of this substituted diazole as antituberculotic.
专利号:US-8129544-B2 优先权日:2002-10-15 标题:1-substituted-4-nitroimidazole compound and method for preparing the same 发明人:GOTO FUMITAKA; TAKEMURA NORIAKI; OTANI TADAAKI; HASEGAWA TAKESHI; TSUBOUCHI HIDETSUGU; UTSUMI NAOTO; FUJITA SHIGEKAZU; KURODA HIDEAKI; SHITSUTA TAKUYA; SASAKI HIROFUMI 权利人:GOTO FUMITAKA; TAKEMURA NORIAKI; OTANI TADAAKI; HASEGAWA TAKESHI; TSUBOUCHI HIDETSUGU; UTSUMI NAOTO; FUJITA SHIGEKAZU; KURODA HIDEAKI; SHITSUTA TAKUYA; SASAKI HIROFUMI; OTSUKA PHARMA CO LTD 摘要:The present invention relates to a 1-substituted-4-nitroimidazole compound represented by the general formula (1) or a salt thereof, n n(wherein R is a hydrogen atom, a lower alkoxy group-substituted lower alkyl group, a phenyl-lower alkoxy group-substituted lower alkyl group, a cyano-substituted lower alkyl group, a phenyl-lower alkyl group which may have lower alkoxy groups as the substituents in the phenyl ring or a group of the formula —CH 2 R A ; X is a halogen atom or a group of the formula —S(O)n-R 1 ) and method for preparing the same. The compound of the formula (1) is a useful compound as an intermediate for synthesis of various pharmaceutical and agricultural chemicals, particularly, as intermediates for antitubercular agents.
专利号:US-2022096575-A1 优先权日:2017-02-14 标 题 :Modulation of microbial synthesis of 4-ethylphenol and 4-ethylphenyl sulfate in behavior and disease
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合成参考文献
参考文献:10.1021/jm1010644 摘要:Cherian J, Choi I, Nayyar A, Manjunatha UH, Mukherjee T, Lee YS, Boshoff HI, Singh R, Ha YH, Goodwin M, Lakshminarayana SB, Niyomrattanakit P, Jiricek J, Ravindran S, Dick T, Keller TH, Dartois V, Barry CE. Structure–Activity Relationships of Antitubercular Nitroimidazoles. 3. Exploration of the Linker and Lipophilic Tail of ((S)-2-Nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazin-6-yl)-(4-trifluoromethoxybenzyl)amine (6-Amino PA-824). J. Med. Chem. 2011 Jul 26;54(16):5639–59. doi: 10.1021/jm1010644.