专利号:US-5039814-A 优先权日:1990-05-02 标 题:Ortho-lithiation process for the synthesis of 2-substituted 1-(tetrazol-5-yl)benzenes 发明人:SHUMAN RICHARD F; KING ANTHONY O; ANDERSON ROBERT K 权利人:MERCK & CO INC 摘要:A process utilizes the tetrazole functional group to direct lithiation at the ortho position of a phenyltetrazole and generate a nucleophilic aryllithium species which then undergoes reaction with an electrophile to generate a 2-substituted 1-(tetrazol-5-yl)benzene. The process is useful in the production of intermediates in the synthesis of angiotensin II antagonists. This novel process is a more cost effective and versatile route for the large-scale preparation of these key intermediates.
专利号:US-9000205-B2 优先权日:2012-08-06 标题:Process for the preparation of 2-cyanophenylboronic acid and esters thereof 发明人:FONTANA FRANCESCO; ROSSI EMILIANO; DE FILIPPO CHRISTIAN 权利人:F I S —FABBRICA ITALIANA SINT S P A 摘要:The present invention relates to a process for the synthesis of 2-cyanophenylboronic acid and the esters and salts thereof of formula (II), which are intermediates of the synthesis of active pharmaceutical ingredients such as Perampanel or E2040. formula (II): (II).
专利号:EP-3560934-A1 优先权日:2018-04-26 标题:Process for the preparation of pure 2-cyanophenylboronic acid and esters thereof, intermediates of perampanel or of e2040 发明人:FONTANA FRANCESCO; DI PIETRO FEDERICO; NALIN ARNALDO 权利人:FIS FABBRICA ITALIANA SINTETICI SPA 摘要:The present invention relates to a process for the synthesis of 2-cyanophenylboronic acid and the esters and salts thereof, which are intermediates of the synthesis of active pharmaceutical ingredients such as Perampanel or E2040, wherein impurity formation, in particular the formation of DBBN iPrketone, is reduced.
专利号:US-7071338-B2 优先权日:2002-11-27 标 题 :Process for the synthesis of bis-aryl diamidoxime compounds 发明人:BOYKIN DAVID W; ANBAZHAGAN MARIAPPAN; TIDWELL RICHARD R 权利人:UNIV GEORGIA STATE RES FOUND 摘要:Bis-aryl diamidoxime compounds, such as 2,5-bis [4-hydroxy and 4-O-alkylamidinophenyl] furans, can be prepared from 2,5-bis tri-alkylstannanes via a one step palladium-catalyzed cross reaction. Bis-aryl diamidoxime compounds, such as 2,5-bis [4-hydroxy and 4-O-alkylamidinophenyl]furans, are useful as therapeutic compounds. The disclosed process is scalable, simpler, more economic and more feasible than other presently known methods of preparing 2,5-bis [4-hydroxy and 4-O-alkylamidinophenyl]furans and other bis-aryl diamidoxime compounds.
专利号:TW-I655905-B 优先权日:2012-07-24 标题 :Contains 4-amino-3-chloro-5-fluoro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylic acid or a derivative thereof and very long chain fatty acid (VLCFA) Synthesis of herbicidal compositions with fatty acid/fat synthesis inhibiting herbicides
专利号:WO-9637481-A1 优先权日:1995-05-26 标题:Novel reagent for tetrazole synthesis and process for producing tetrazoles therewith 发明人:TOKUHARA GINRO; YAMAGUCHI TADASHI; IWASAKI TETSUYA 权利人:CHUGOKU KAYAKU; WAKUNAGA SEIYAKU KK; TOKUHARA GINRO; YAMAGUCHI TADASHI; IWASAKI TETSUYA 摘要:A process for producing 1H-tetrazoles represented by general formula (II) (wherein R represents an arbitrary substituent) from carbonitriles represented by the general formula (I): R-CN (wherein R is as defined above) with the use of a tetrazolating agent comprising an alkali metal azide and zinc chloride. The agent can be used in a variety of solvents and can fundamentally be applied to any carbonitriles. As zinc chloride is inexpensive, it contributes to cost reduction.
摘要:Black, D. A.; Fagnou, K., Science of Synthesis, (2010) 45, 555. 摘要:Black, D. A.; Fagnou, K., Science of Synthesis, (2010) 45, 589. 摘要:Alonso, D. A.; Nájera, C., Science of Synthesis, (2010) 47, 473. 摘要:Li, Y.; Xie, W.; Jiang, X., Science of Synthesis Knowledge Updates, (2016) 2, 8. 摘要:Bertus, P.; Boeda, F.; Pearson-Long, M. S. M., Science of Synthesis Knowledge Updates, (2012) 1, 41.