专利号:WO-9517903-A1 优先权日:1993-12-28 标 题:Modular design and synthesis of oxazolone-derived molecules 发明人:HOGAN JOSEPH C JR; CASEBIER DAVID; FURTH PAUL; TU CHENG 权利人:ARQULE PARTNERS L P; HOGAN JOSEPH C JR; CASEBIER DAVID; FURTH PAUL; TU CHENG 摘要:The design and synthesis of novel oxazolone-derived molecular modules and the use of the modules in the construction of new molecules and fabricated materials is disclosed. The new molecules and fabricated materials are molecular recognition agents useful in the design and synthesis of drugs, and have applications in separations and materials science.
专利号:US-5041637-A 优先权日:1988-07-12 标题:Process for the synthesis of optically active aminoacids 发明人:CANNATA VINCENZO; TAMERLANI GIANCARLO; CALZOLARI CLAUDIO 权利人:PRESIDENZA DEL CONSIGLIO DEL M 摘要:New process for the synthesis of optically active aminoacids of formula ##STR1## by treating compounds of formula ##STR2## which an optically active alcohol of formula n n R.sub.4 --OH (III) n n n d or 1 n n To obtain a pair of diastereoiosmer esters of formula ##STR3## which is resolved in basic medium into the single diastereoisomer esters of formula ##STR4## from which the desired optically active aminoacid of formula (I) is obtained by treatment in acid medium.
专利号:US-8703996-B2 优先权日:2010-03-09 标题:Short synthesis of tolterodin, intermediates and metabolites 发明人:STERK DAMJAN 权利人:STERK DAMJAN; LEK PHARMACEUTICALS 摘要:A process is described for the preparation of intermediates which can be used for preparation of agents for urinary incontinence therapy, specifically to 2-(3-(diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenol and its prodrugs.
专利号:WO-2017214534-A1 优先权日:2016-06-10 标 题:Synthesis of the arylomycin macrocyclic core 发明人:ROMESBERG FLOYD E; BARAN PHIL; PETERS DAVID 权利人:SCRIPPS RESEARCH INST 摘要:The invention provides a copper-mediated process for making compounds according to Formula (I): that are the macrocyclic scaffolds of the arylomycin class of biologically active compounds, where R 1 , R 2 , R 3 , R A1 , R A2 , R A3 , B, G 1 , G 2 , PG, n2, and n3 are defined in the specification.
专利号:WO-9856944-A1 优先权日:1997-06-10 标 题 :APPLICATION OF REDUCING SULPHUR COMPOUNDS DURING ENZYMATIC PREPARATION OF β-LACTAM COMPOUNDS 发明人:WILMS JOHANNES; DE VROOM ERIK 权利人:GIST BROCADES BV; WILMS JOHANNES; VROOM ERIK DE 摘要:Disclosed is a method to improve the quality of enzymatic hydrolysis or synthesis of the substituted β-lactam compounds with respect to enzyme productivity, product quality and process streamlining (prevention of the formation deposits) by the addition of reducing sulphur compounds, such as sodium sulphite or sodium metabisulphite.
专利号:US-4111933-A 优先权日:1976-04-30 标题:Protection of functional groups during reaction and their subsequent restoration 发明人:ECKERT HEINER; UGI IVAR; KABBE HANS-JOACHIM 权利人:BAYER AG 摘要:In the process for preparing an organic compound of the formula n n A' -- X n n in which n X is an amino group, a hydroxyl group or a carboxyl group, and n A' is the remainder of the molecule, from an organic compound of the formula n n A -- X n n in which n A is the remainder of the molecule which can undergo reaction to form A', by converting A -- X into a compound of the formula n n A -- Z -- COOR n n in which n Z is --NH--, --O-- or a direct C--C bond, and n R is a radical of the formula ##STR1## IN WHICH Y is a direct C--C single bond, the --CHâ•?CH-- group or an arylene group, n R 1 to R 4 each independently is hydrogen, halogen or an alkyl, aryl, aralkyl, alkoxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl or cycloalkylaminocarbonyl radical, or n R 1 + r 2 and R 3 + R 4 each independently completes a 5- or 6-membered carbocyclic ring, or n R 1 and R 3 conjointly with the grouping --C--Y--C-- forms a carbocyclic ring with 5 or 6 carbon atoms, and Hal is halogen, n Thereby to protect X, then converting A -- Z -- COOR into a compound of the formula n n A' -- Z -- COOR n n and then treating the compound A' -- Z -- COOR to restore the group X, the improvement which comprises effecting the treatment of the compound A' -- Z -- COOR with an alkali metal compound of a complex of monovalent cobalt. The process is applicable particularly to aminocarboxylic acids including intermediates from various stages of the synthesis of penicillins and cephalosporis.
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合成参考文献
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