专利号:US-2013338369-A1 优先权日:2011-03-07 标 题 :Process for the Synthesis of Aminobiphenylene 发明人:HEINRICH MARKUS; PRATSCH GERALD 权利人:HEINRICH MARKUS; PRATSCH GERALD; BASF SE 摘要:The present invention relates to a process for the synthesis of 2-aminobiphenylene and derivatives thereof by reacting a benzene diazonium salt with an aniline compound under basic reaction conditions.
专利号:US-10570114-B2 优先权日:2016-05-19 标题:Synthesis of 6-aryl-4-aminopicolinates and 2-aryl-6-aminopyrimidine-4-carboxylates by direct suzuki coupling 发明人:FISK JASON S; LI XIAOYONG; Muehlfeld Mark; BAUMAN ROBERT S; OPPENHEIMER JOSSIAN; TU SIYU; NITZ MARK A; CHAKRABARTI REETAM; FEIST SHAWN D; RINGER JAMES W; LENG RONALD B 权利人:DOW AGROSCIENCES LLC 摘要:Improved methods of synthesizing 6-aryl-4-aminopicolinates, such as arylalkyl and alkyl 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylates and arylalkyl and alkyl 4-amino-3-chloro-5-fluoro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylates, are described herein. The improved methods include a direct Suzuki coupling step, which eliminates the protection/de-protection steps in the current chemical process, and therefore eliminates or reduces various raw materials, equipment and cycle time as well as modification of other process conditions including use of crude AP, use of ABA-diMe, and varying pH, catalyst concentration, solvent composition, and/or workup procedures. This includes synthesis of 2-aryl-6-aminopyrimidine-4-carboxylates.
专利号:US-2008280855-A1 优先权日:2005-06-22 标 题 :Process For the Production of Intermediates For the Preparation of Tricyclic Benzimidazoles 发明人:CHIESA MARIA VITTORIA; PALMER ANDREAS; BUHR WILM; ZIMMERMANN PETER JAN; BREHM CHRISTOF; SIMON WOLFGANG-ALEXANDER; POSTIUS STEFAN; KROMER WOLFGANG; ZANOTTI-GEROSA ANTONIO 权利人:NYCOMED GMBH 摘要:The invention relates to a process for the synthesis of compounds of the formula 1-a and compounds of the formula 1-b. n n n n n n n n n n The compounds of the formula 1-a and the compounds of the formula 1-b, in which the substituents R1, R2, R3, and Ar have the meanings indicated in the description, are valuable intermediates for the preparation of pharmaceutically active compounds.
专利号:US-2023174490-A1 优先权日:2020-03-18 标 题 :Improved synthesis of 6-aryl-4-aminopicolinates 发明人:ZHANG CHUNMING; TU SIYU; LENG RONALD B; IRVINE NICHOLAS; SCHUITMAN ABRAHAM; SHINKLE AARON; DEVARAJ JAYACHANDRAN; ZU CHENGLI 权利人:CORTEVA AGRISCIENCE LLC 摘要:The present disclosure relates to improved methods of synthesizing 6-aryl-4-aminopicolinates, such as arylalkyl and alkyl 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylates.
专利号:US-7812161-B2 优先权日:2007-03-05 标 题 :Synthesis of GlyT-1 inhibitors 发明人:PFLEGER CHRISTOPHE; WALDMEIER PIUS; WANG SHAONING 权利人:HOFFMANN LA ROCHE 摘要:The present invention relates to a process for preparation of a compound of formula I n nwhereinn Het, R 1 , R 2 , R 3 , and n are as defined herein and pharmaceutically acceptable acid addition salts thereof, which comprises reacting a compound of formula 21 with a compound of formula 8 to obtain a compound of formula 11 and coupling the compound of formula 11 in the presence of a coupling reagent or the corresponding acid halogenide with a compound of formula 15 to obtain a compound of formula I.
专利号:US-3992456-A 优先权日:1969-04-16 标题:Synthesis of alkadienols 发明人:ATKINS KENNETH EARL; MANYIK ROBERT MICHAEL; O'CONNOR GEORGE LAWRENCE 权利人:UNION CARBIDE CORP 摘要:Alkadienols are prepared by reacting a conjugated diolefin, such as butadiene, with water in the presence of palladium or platinum catalyst and in the presence of solvents. The addition of carbon dioxide to the reaction mixture greatly increases the yield of alkadienols. The products can be hydrogenated to saturated alcohols, useful for making plasticizers.
[参考文献]: Heng Zhang, Et Al. Synthesis And Evaluation Of Fluorine-Substituted Phenyl Acetate Derivatives As Ultra-Short Recovery Sedative/hypnotic Agents. Plos One. 2014 May 5;9(5):E96518.