3,4-二甲氧基苯胺置于盐酸,Sodium Nitrite,四羟基二硼体系中,用 甲醇,水 用作溶剂,化学反应 1.5H,以65%的收率获得3,4-二甲氧基苯硼酸 参考文献:Methanol-Promoted Borylation Of Arylamines: A Simple And Green Synthetic Method To Arylboronic Acids And Arylboronates 标题:Methanol-Promoted Borylation Of Arylamines: A Simple And Green Synthetic Method To Arylboronic Acids And Arylboronates 摘要:A Sandmeyer Borylation Of Arylamines Via A Sn2Ar Pathway Promoted By Methanol With Sodium Nitrite And Hydrochloric Acid As Diazotization Agent Has Been Developed,Which Provide A Simple And Green Synthetic Method To Arylboronic Acids And Arylboronates. Doi:10.1055/s-0033-1339118
专利号:US-2006287529-A1 优先权日:2003-02-20 标 题:Solid phase synthesis of antitumoral compounds 发明人:ALVAREZ MERCEDES; ALBERICIO FERNANDO; CIRONI PABLO; CUE VAS CARMEN; FRANCESCH ANDREAS; MARFIL MARTA 权利人:ALVAREZ MERCEDES; ALBERICIO FERNANDO; CIRONI PABLO; CUE VAS CARMEN; FRANCESCH ANDREAS; MARFIL MARTA 摘要:Lamellarins are prepared using a solid phase synthesis. In a first aspect, the process includes a step as follows: Formula (I) where R 1 to R 15 are as defined, and X is halogen, provided that one of R 2 , R 3 or R 4 is immobilised to a resin. In a second aspect, the process includes a step as follows: Formula (II) where R 1 ′ to R 5 ′, R 11 ′ and R 13 ′ are as defined, X 1 and X 2 are halogen, M is a metal function and PG is an amino protecting group, provided that one of that R 2 ′, R 3 ′ or R 4 ′ is immobilised to a resin.
专利号:US-9085511-B2 优先权日:2011-04-04 标题:Atropisomeric 1,8-bisphenolnapthalenes and their use in enantioselective recognition and asymmetric synthesis 发明人:WOLF CHRISTIAN; GHOSN MARWAN 权利人:WOLF CHRISTIAN; GHOSN MARWAN; UNIV GEORGETOWN 摘要:This invention related to atropisomeric 1,8-bisphenolnaphthalenes and derivatives thereof of the general formula (I): n nwhich are useful in resolution of enantiomers, enantioselective recognition and asymmetric synthesis.
专利号:US-2023365629-A1 优先权日:2018-06-15 标题:Synthesis of echinocandin antifungal agent
专利号:EP-1836163-B1 优先权日:2004-12-23 标题 :Pyrrolidine derivatives for the treatment of a disease depending on the activity of renin 发明人:BREITENSTEIN WERNER; COTTENS SYLVAIN; EHRHARDT CLAUS; JACOBY EDGAR; LORTHIOIS EDWIGE LILIANE JEANNE; MAIBAUM JUERGEN KLAUS; OSTERMANN NILS; SELLNER HOLGER; SIMIC OLIVER 权利人:NOVARTIS AG 摘要:Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on inappropriate activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described. The substituted pyrrolidine compounds are especially of the formula I wherein the substituents are as described in the specification.
专利号:EP-1613635-A2 优先权日:2003-02-20 标题 :Solid phase synthesis of antitumoral compounds
专利号:US-11524980-B2 优先权日:2018-06-15 标 题 :Synthesis of echinocandin antifungal agent
摘要:Yoshikai, N.; Rayner, C. M.; Graham, M. A., Science of Synthesis Knowledge Updates, (2020) 2, 79. 摘要:Tomé, A. C., Science of Synthesis Knowledge Updates, (2015) 2, 89. 摘要:Sato, N., Science of Synthesis Knowledge Updates, (2011) 4, 293. 摘要:Beier, P., Science of Synthesis Knowledge Updates, (2014) 2, 307. 摘要:Guram, A. S.; Milne, J. E.; Tedrow, J. S.; Walker, S. D., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 102.