2085-88-3 = 1123-85-9 + 93-53-8 反应条件:1.1 Catalysts: Iridium(1+),[(1,2,5,6-η)-1,5-Cyclooctadiene]Hydro[(8-Quinolinyl-Kn)Methyl-Kc](T... Solvents: Tetrahydrofuran; 23 °C; 22 H,85 °C 标题:An Air-Stable Cationic Iridium Hydride As A Highly Active And General Catalyst For The Isomerization Of Terminal Epoxides 作者:Humbert,Nicolas; Vyas,Devendra J.; Besnard,Celine; Mazet,Clement 参考文献:Chemical Communications (Cambridge 日期:2014 卷标:50(73) 页码:10592-10595
专利号:US-6600040-B2 优先权日:2000-06-08 标 题:Process for the synthesis of (2R, 2-alpha-R, 3A)-2-[1-(3,5-bis(trifluoromethyl)phenyl)ethoxy]-3-(4-fluorophenyl)-1, 4-oxazine 发明人:BRANDS KAREL M JOS; TSAY FUH-RONG; CONRAD KAREN M; ZHAO MATTHEW M 权利人:MERCK & CO INC 摘要:The present invention is concerned with novel processes for the preparation of (2R, 2-alpha-R, 3a)-2-[1-[3,5-bis(trifluoromethyl)phenyl]ethoxy-3-(4-fluorophenyl)-1,4-oxazine. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
专利号:US-6469164-B2 优先权日:2000-06-08 标题:Process for the synthesis of (2R, 2-alpha-R)-4-benzyl-2-[1-(3,5-bis (trifluoromethyl)phenyl)ethoxy]-1,4-oxazine-3-one 发明人:BRANDS KAREL M JOS; PAYACK JOSEPH F; PYE PHILIP J 权利人:MERCK & CO INC 摘要:The present invention is concerned with novel processes for the preparation of (2R, 2-alpha-R)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]ethoxy-1,4-oxazin-3-one. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
专利号:US-2008242866-A1 优先权日:2007-03-30 标 题 :Synthesis of anthranilamides 发明人:SCHMEES NORBERT; PETROV ORLIN 权利人:SCHMEES NORBERT; PETROV ORLIN 摘要:The present invention relates to a novel method of preparing anthranilamides of formula I: n n n n n n n n n n in which R 1 , R 2 , R 3 , A, E, Q, X, and W are defined in the claims, to a novel intermediate compound, and to the use of said novel intermediate compound for the preparation of said anthranilamides of formula I.
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-8455655-B2 优先权日:2010-05-07 标题:Preparation of dihydropyridines 发明人:VISHNU NEWADKAR RAVINDRANATH; PURUSHOTTAM JOSHI ANIL; KUMAR SINGH SANTOSH 权利人:VISHNU NEWADKAR RAVINDRANATH; PURUSHOTTAM JOSHI ANIL; KUMAR SINGH SANTOSH; LESVI LABORATORIOS SL 摘要:The invention relates to a method and compounds for the preparation of clevidipine butyrate, a very short acting hypertensive calcium antagonist, as well as the synthesis of these compounds useful for the preparation of clevidipine (also known as clevidipine butyrate). Moreover the invention also discloses polymorphic forms of clevidipine butyrate, useful for the preparation of pharmaceutical compositions, and processes to prepare them.
专利号:US-4980291-A 优先权日:1988-02-10 标 题 :Process for the enzymatic separation of the optical isomers of racemic α-alkyl-substituted primary alcohols 发明人:BIANCHI DANIELE; CESTI PIETRO; FRANCALANCI FRANCO; CABRI WALTER 权利人:DONEGANI GUIDO IST 摘要:Biotechnological resolution by means of enzymatic transesterification of the relevant racemic mixture of the optical isomers of α-alkyl-substituted primary alcohols having the formula (I): ##STR1## wherein: R represents a linear or branched (C 1 -C 20 )-alkyl or alkenyl group or an aryl group, also substituted or condensed with other groups, in particular a group of formula (II) or (III): ##STR2## wherein: R ii represents a (C 1 -C 8 )-alkyl group, a (C 1 -C 4 )-alkenyl group, an alkoxy, phenyl, phenoxy, benzoyl, or heterocyclic group; n R iii represents a hydrogen or halogen atom; n R iv represents a (C 1 -C 4 )-alkyl group, n and wherein n R i represents a (C 1 -C 4 )-alkyl group either equal to, or different from, R, n in the presence of an enzyme either free or immobilized on a support capable of selectively causing the S isomer to be esterified, with the R isomer being left substantially unchanged, said isomers being then separated according to techniques known from the prior art. The process is used in the synthesis of antiinflammatory agents.
[参考文献]: I F Gaunt, Et Al. Short-Term Toxicity Of 2-Phenylpropan-1-Ol (Hydratropic Alcohol) In Rats. Food Chem Toxicol. 1982 Oct;20(5):519-25. [参考文献]: S Goenechea, Et Al. [参考文献]: Z Rechtsmed. 1986;97(2):83-8. [参考文献]: W Gielsdorf, Et Al. [参考文献]: Z Rechtsmed. 1982;89(3):191-5.
合成参考文献
摘要:Chciuk, T. V.; Flowers, R. A.; Flowers, R. A., Science of Synthesis Knowledge Updates, (2016) 2, 236. 摘要:Brown, J. M.; Nguyen, B. N., Science of Synthesis: Stereoselective Synthesis, (2011) 1, 295. 摘要:Stoltz, B.; Ebner, D. C.; Park, N., Science of Synthesis: Stereoselective Synthesis, (2011) 2, 224. 摘要:Wu, X.; Xiao, J., Science of Synthesis: Water in Organic Synthesis, (2012) 1, 257. 摘要:Wu, X.; Xiao, J., Science of Synthesis: Water in Organic Synthesis, (2012) 1, 268.