专利号:WO-2024151344-A9 优先权日:2022-11-18 标题:A device that enables the combinatorial synthesis of small molecule libraries 发明人:COPELAND Gregory; LIU JANE 权利人:BRT BIOTECHNOLOGIES INC 摘要:A device for the synthesis of small molecules on a substrate is provided. The device includes a synthesis plate with vias, and a microfluidic patterning plate with a series ot open-faced channels that can be aligned with the vias on the synthesis plate. The device may be used to synthesize combinatorial libraries of small molecules.
专利号:US-7612210-B2 优先权日:2005-12-05 标题:Process for selective synthesis of enantiomers of substituted 1-(2-amino-1-phenyl-ethyl)-cyclohexanols 发明人:MAHANEY PAIGE ERIN; ANTANE MADELENE MIYOKO; SUN JERRY SHUNNENG 权利人:WYETH CORP 摘要:A process for the enantioselective synthesis of an (S)- or (R)-1-[2-dimethylamino)-1-(methoxyphenyl)ethyl]cyclohexanol and analogues or salt thereof are described. The method involves the steps of (a) reacting an (S) or (R) 4-benzyloxazolidinone with a mixed anhydride of a methyoxyphenylacetic acid under conditions which form a oxazolidinone, (4S)- or (4R)-4-benzyl-3-[methyoxyphenyl]acetyl]-oxazolidin-2-one, (b) treating the (4S)- or (4R)-4-benzyl-3-[(methoxyphenyl)acetyl]-1,3-oxazolidin-2-one with an aprotic amine base and titanium chloride in a chlorinated solvent under conditions which permit formation of the corresponding anion, (c) mixing the corresponding anion with titanium chloride and cylcohexanone under conditions which permit an aldol reaction to form the corresponding (4S)- or (4R)-4-benzyl-3-[(2R)-2-(1-hydroxycyclohexyl)-2-(methoxyphenyl)acetyl]-1,3-oxazolidin-2-one,(d) hydrolyzing the (4S)— or (4R)-4-benzyl-3-[(2R)-2-(1-hydroxycyclohexyl)-2-(methoxyphenyl)acetyl]-1,3-oxazolidin-2-one to form a chiral acid (2S or 2R)-(1-hydroxycyclohexyl)-methoxyphenyl)acetic acid, (e) coupling the chiral phenylacid to a secondary amine to form an amide, and (f) reducing the amide to form an (S) or (R) 1[2-dimethylamino)-1-(methoxyphenyl)ethyl]cyclohexanol or a salt thereof.
专利号:US-2003083352-A1 优先权日:2000-07-31 标 题 :Synthesis of imidazole intermediates 发明人:HELAL CHRISTOPHER J 权利人:PFIZER 摘要:The invention provides a method for synthesis of compounds of formula n n n wherein R 1 and R 19 are as defined. Compounds of formula 12 are useful as intermediates for synthesizing compounds having pharmacological activity inhibiting cdk5, cdk2, and GSK-3.
专利号:US-4824532-A 优先权日:1987-01-09 标题:Process for the electrochemical synthesis of carboxylic acids 发明人:MOINGEON MARIE-ODILE; CHAUSSARD JACQUES; TROUPEL MICHEL; SABOUREAU CHRISTOPHE 权利人:AEROSPATIALE 摘要:The invention relates to a process for the electrosynthesis of carboxylic acids of general formula R-COOH in which R is an organic radical by the electrochemical reduction, in the presence of carbon dioxide, of organic compounds corresponding to the general formula R-Y in which R is the above-mentioned organic radical and Y is a hetero atom-containing radical, the hetero atom of the radical Y, chosen from the group consisting of oxygen, nitrogen, sulphur andphosphorus, being directly linked to a carbon atom of the radical R by a single covalent linkage. When the hetero atom is nitrogen or phosphorus, the radical Y is an ammonium or phosphonium radical respectively. The anode, which is consumed during the electrosynthesis, is made of a metal chosen from the group consisting of reducing metals and their alloys, preferably made of magnesium, aluminium or zinc. This process without catalyst is very simple to perform and enables a cell with a single compartment to be employed. The carboxylic acids are commonly employed in the chemical industry, especially as intermediates for the synthesis of pharmaceutical products or of products used in plant protection.
专利号:US-9409855-B2 优先权日:2012-07-25 标 题 :Asymmetric synthesis of (−)-venlafaxine using organocatalyst 发明人:CHAVAN SUBHASH PRATAPRAO; GARAI SUMANTA; PAWAR KAILASH PRALHAD 权利人:COUNCIL SCIENT IND RES 摘要:The patent discloses an asymmetric synthesis of (−)-venlafaxine using an organocatalyst via a unified strategy employing organcatalytic Michael addition, regio-selective dehydration and selective epoxide ring opening.
专利号:US-9206222-B2 优先权日:2009-06-29 标题:Solid phase peptide synthesis of peptide alcohols 发明人:CAUSSIL-AMBLARD MURIEL; MARTINEZ JEAN; TAILHADES JULIEN 权利人:CAUSSIL-AMBLARD MURIEL; MARTINEZ JEAN; TAILHADES JULIEN; CENTRE NAT RECH SCIENT 摘要:The present invention relates to the synthesis of depsipeptides on solid phase support. Said depsipeptides are then implicated in a solution phase O—N acyl shift enabling to obtain the corresponding peptide alcohols.
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合成参考文献
摘要:Zhou, Q.-Q.; Wei, Y.; Lu, L.-Q.; Xiao, W.-J., Science of Synthesis: Photocatalysis in Organic Synthesis, (2018) 1, 204. 摘要:Sawamura, M.; Shimizu, Y., Science of Synthesis: Knowledge Updates, (2024) 2, 201. 摘要:Das, A.; Ramkumar, N.; Veliks, J., Science of Synthesis: Modern Strategies in Organofluorine Chemistry, (2025) 2.