专利号:WO-2012017400-A1 优先权日:2010-08-03 标 题 :Synthesis of acyl-pantetheine derivatives and the use thereof in the synthesis of acyl-coenzyme a derivatives 发明人:VAN DIJK ALBERDINA AIKE; BADENHORST CHRISTOFFEL PETRUS STEPHANUS 权利人:UNIV NORTHWEST; VAN DIJK ALBERDINA AIKE; BADENHORST CHRISTOFFEL PETRUS STEPHANUS 摘要:The present invention relates to a novel synthesis method for acyl-pantetheine derivatives. The present invention further relates to the use of said synthesized acyl-pantetheine derivatives as a starting material in the enzymatic synthesis of acyl-coenzyme A derivatives. According to a first aspect thereof, the present invention provides a method for the synthesis of acyl-pantetheine derivatives, the method including the steps of: a) providing a source of pantetheine; b) providing a source of acyl ester; and c) contacting the source of pantetheine with the source of acyl ester to form the corresponding acyl-pantetheine derivative, having the general formula (I), wherein R is an acyl group.The present invention also provides a method for the synthesis of acyl-coenzyme A derivatives as well as the use of a source of pantetheine and a source of acyl ester in the preparation steps of these two methods.
专利号:WO-2009104605-A1 优先权日:2008-02-18 标 题 :Novel intermediate for synthesis of ascofranone having various physiological activities, and novel shortened total synthesis method for ascofranone using the same 发明人:SAIMOTO HIROYUKI; HAGA YASUSHI 权利人:ARIGEN PHARMACEUTICALS INC; SAIMOTO HIROYUKI; HAGA YASUSHI 摘要:In the synthesis of ascofranone, a compound represented by formula (III), (IV), (V) or (VII) or an optical isomer thereof is used as an intermediate for the synthesis. [In the formulae, R 1 and R 2 independently represent a hydrogen atom, a C 1-7 alkyl group, a phenoxyalkyl group having a halogen atom on a carbon atom in a benzene ring therein, or a phenyl group having a C 1-7 alkoxy group or a C 1-7 alkoxycarbonyl group on a carbon atom in a benzene ring therein; and X represents a halogen atom or a group R 5 SO 3 (wherein R 5 represents a C 1-7 alkyl group or a phenyl group having a C 1-7 alkyl group on a carbon atom in a benzene ring therein).] By using the compound, it becomes possible to reduce the number of steps required for the total synthesis of ascofranone to 7 or 8 from 12 which is a number of the steps required for the conventional ascofranone total synthesis processes.
专利号:US-2010099894-A1 优先权日:2006-10-09 标 题 :Method for the Synthesis of Cyclic Acetals by the Reactive Extraction of a Polyol in a Concentrated Solution 发明人:DUBOIS JEAN-LUC; IBORRA CHORNET SARA; VELTY ALEXANDRA I LUCIENNE; CORMA CANOS AVELINO 权利人:DUBOIS JEAN-LUC; IBORRA CHORNET SARA; VELTY ALEXANDRA I LUCIENNE; CORMA CANOS AVELINO 摘要:A method for the synthesis of cyclic acetals comprises reacting at least one carbonyl-function compound selected from aldehydes, ketones, and/or linear acetals, on a polyol in a concentrated aqueous solution exceeding 20 wt % in a reactor containing an acidic catalyst. The carbonyl-function compound is selected so that the cyclic acetal obtained has a water solubility lower than 20000 mg/kg. During the catalytic reaction for the cyclic acetal synthesis, at least one portion of the organic phase containing the cyclic acetal is separated. The acidic catalysis is either homogeneous when using a water-soluble strong acid, or heterogeneous when using a solid acid such as a resin, a zeolite, or any appropriately acidified solid. The extractive reaction method can be used for obtaining high conversions and selectivity.
专利号:WO-2018157416-A1 优先权日:2017-02-28 标题 :Process for synthesis of 3,3,3-trifluropropyl dimethylsilyl propylene ether 发明人:SI LINXU; LI JIAQI; JU CHAOFAN; WU JUNYI 权利人:CHANGSHU 3F ZHONGHAO NEW CHEMICAL MAT CO LTD; NEIMENGGU ALLTOP FLUORINE NEW MAT DEVELOPMENT CO LTD 摘要:Disclosed is a process for the synthesis of 3,3,3-trifluropropyl dimethylsilyl propylene ether, the process comprising the following steps: (1) dimethyl monochlorosilane and propylene alcohol are added into a reactor, and a triethylamine catalyst and an n-hexane reaction solvent are then added, wherein the reaction process requires stirring, and during the process, a constant temperature oil bath is used for heating, and nitrogen is introduced; (2) after the reaction is completed, the product is left to stand for layering, and triethylamine hydrochloride in the lower layer is discharged to obtain crude 3,3,3-trifluropropyl dimethylsilyl propylene ether; and (3) the filtered crude 3,3,3-trifluropropyl dimethylsilyl propylene ether is rectified under a reduced pressure to obtain a high-purity 3,3,3-trifluropropyl dimethylsilyl propylene ether product. The 3,3,3-trifluropropyl dimethylsilyl propylene ether synthesized by the present invention has a lower raw material price, milder reaction conditions, and a safe and reliable reaction process; furthermore, the synthesis process is simple, has fewer side reactions, and produces less waste, wherein same is easy to treat, and the target product is easy to separate and has a high purity.
专利号:US-5145957-A 优先权日:1988-03-18 标 题:Stereoselective synthesis of a chiral cis 3-beta hydrogen (3R) 4-aroyloxy azetidinone 发明人:TSCHAEN DAVID M; LYNCH JOSEPH E; LASWELL WILLIAM L; VOLANTE RALPH P; SHINKAI ICHIRO 权利人:MERCK & CO INC 摘要:A process is described for the stereocontrolled synthesis of (3R,4R)-3-[(1R)-1-hydroxyethyl]-4-benzoyloxyazetidin-2-ones and their derivatives by cycloaddition involving an imine and a ketone, generated from 3(S)-hydroxybutyrate which are useful intermediates in the synthesis of carbapenem antibiotics.
专利号:US-5817751-A 优先权日:1994-06-23 标 题 :Method for synthesis of diketopiperazine and diketomorpholine derivatives 发明人:SZARDENINGS ANNA KATRIN; CAMPBELL DAVID 权利人:AFFYMAX TECH NV 摘要:The present invention relates to the areas of organic and medicinal chemistry. More specifically, the present invention is concerned with combinatorial and solid phase methods for the synthesis of diverse diketopiperazine derivatives, and the use of such methods to create libraries of diverse diketopiperazine derivatives. The present invention has application in the areas of chemical synthesis, the screening for new diketopiperazine derivatives having beneficial medical properties and the use of such screening to provide compositions and methods including diketopiperazine derivatives for treating disease.
参考文献:10.1107/s1600536811016631 摘要:Xu H, Sun HS, Luo FM, Ding JQ. 1-Butyl-3-(1-naphtho-yl)-1H-indole. Acta Crystallogr Sect E Struct Rep Online. 2011 Jun 01;67(Pt 6):o1349. 参考文献:10.1016/j.bmcl.2011.06.034 摘要:Xiao X, Wu J, Trigili C, Chen H, Chu JWK, Zhao Y, Lu P, Sheng L, Li Y, Sharom FJ, Barasoain I, Diaz JF, Fang W. Effects of C7 substitutions in a high affinity microtubule-binding taxane on antitumor activity and drug transport. Bioorganic & Medicinal Chemistry Letters. 2011 Aug;21(16):4852–6. doi: 10.1016/j.bmcl.2011.06.034.