专利号:US-10711138-B2 优先权日:2016-04-08 标题:Intermediates and procedures for the synthesis of functional materials 发明人:KIRSCH PEER; GUNST SUSANN 权利人:MERCK PATENT GMBH 摘要:The present invention relates to heteroaromatic compounds which have two different reactive groups, their use in the synthesis of asymmetrically substituted compounds, and synthesis processes in which the compounds according to the invention are reacted sequentially with two different compounds, whereby an asymmetrically substituted compound is formed.
专利号:US-9126995-B2 优先权日:2011-11-08 标题:Method for catalytic asymmetric synthesis of optically active isoxazoline compound and optically active isoxazoline compound 发明人:TOYAMA KEN-ICHI; MORIYAMA YUJI; MATOBA KAZUTAKA; YAOSAKA MANABU; IKEDA EITATSU 权利人:NISSAN CHEMICAL IND LTD 摘要:There is provided a method for catalytic asymmetric synthesis of optically active isoxazoline compound and an optically active isoxazoline compound. A method for catalytic asymmetric synthesis of optically active isoxazoline compound of a formula (6) including reacting an α,β-unsaturated carbonyl compound of a formula (1) and a hydroxylamine in a solvent in the presence of a base by adding a chiral phase transfer catalyst. An optically active isoxazoline compound of a formula (13) that can be synthesized by the method.
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-7767826-B2 优先权日:2007-10-05 标题 :Process for the synthesis of L-(+)-ergothioneine 发明人:TRAMPOTA MIROSLAV 权利人:PHARMATECH INTERNATIONAL INC 摘要:This invention relates to a novel process for the preparation of optically pure L-(+)-ergothioneine. The process for the chemical synthesis of L-ergothioneine comprises steps which consist of reacting L-histidine alkyl ester with an acid halide, chloroformate or pyrocarbonate in the presence of a base, hydrolysis of the alkyl-(S,Z)-2,4,5-triamidopent-4-enoate to obtain a (S)-alkyl 2,5-diamido-4-oxopentanoate, acid catalyzed hydrolysis of the (S)-alkyl 2,5-diamido-4-oxopentanoate followed by reaction with a metal thiocyanate to obtain the thiohistidine, protection of the sulfur of thiohistidine as the tert-butyl thioether, dialkylation of the primary amine to obtain a tertiary amine, quaternization of the tertiary amine, and removal of the protecting group to obtain the desired (S)-3-(2-mercapto-1H-imidazol-5-yl)-2-(trialkylammonio)propanoate (I). This process affords a better yield and is capable of practical application at large scale.
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-2006058532-A1 优先权日:2004-09-10 标 题:Process for the scalable synthesis of 1,3,4,9-tetrahydropyrano[3,4-b]-indole derivatives 发明人:CHEW WARREN; CHEAL GLORIA K; LUNETTA JACQUELINE F; DEMERSON CHRISTOPHER A 权利人:CHEW WARREN; CHEAL GLORIA K; LUNETTA JACQUELINE F; DEMERSON CHRISTOPHER A 摘要:The invention is directed to a process of synthesizing compounds of formula (VI): n n nwherein R 1- R 9 , R 3′ , R 4′ and Y are as set forth in the specification, and said method is useful for large scale synthesis thereof. The invention is also directed to useful intermediates for synthesizing the compounds of formula (VI) and processes of preparing said intermediates.
摘要:Malins, L. R.; Payne, R. J., Science of Synthesis Knowledge Updates, (2021) 3, 195. 摘要:Adriaensen, K.; De Vos, D., Science of Synthesis, (2022) , 167. 参考文献:10.1021/ja502806r 摘要:Thompson RE, Liu X, Alonso-García N, Pereira PJ, Jolliffe KA, Payne RJ. Trifluoroethanethiol: an additive for efficient one-pot peptide ligation-desulfurization chemistry. J Am Chem Soc. 2014 Jun 11;136(23):8161–4. doi: 10.1021/ja502806r.