专利号:US-5698741-A 优先权日:1995-05-25 标题 :Asymmetric synthesis of (-)6-chloro-4-cyclopropyl-ethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one 发明人:THOMPSON ANDREW S; CORLEY EDWARD G; GRABOWSKI EDWARD J J; YASUDA NOBUYOSHI 权利人:MERCK & CO INC 摘要:An improved synthesis of a highly potent HIV reverse transcription inhibitor is disclosed, involving an acetylide and a trifluoromethyl ketone which produces a chiral product in the presence of a chiral amino alcohol.
专利号:US-5663467-A 优先权日:1995-01-23 标题:Synthesis of cyclopropylacetylene 发明人:THOMPSON ANDREW S; CORLEY EDWARD G; HUNTINGTON MARTHA 权利人:MERCK & CO INC 摘要:An improved synthesis of cyclopropylacetylene involving cyclization of 5-halo-1-pentyne in strong base is disclosed, and is useful for preparing compounds with a cyclopropylethynyl substituent, such as an intermediate for a highly potent HIV reverse transcriptase inhibitor or other pharmaceutically active compounds.
专利号:US-12133887-B2 优先权日:2018-12-18 标题 :Chemical synthesis of oligosaccharides of Pseudomonas aeruginosa serotype O11 O-antigen 发明人:YIN JIAN; HU JING; LIU ZHONGHUA; QIN CHUNJUN 权利人:UNIV JIANGNAN 摘要:The disclosure discloses a chemical synthesis method of oligosaccharides of a Pseudomonas aeruginosa serotype O11 O-antigen, and belongs to the field of chemistry. The disclosure includes constructing an O-antigen trisaccharide by using a D-glucose building block, an L-fucosamine building block and a D-fucosamine building block; wherein the D-glucose building block or the L-fucosamine building block is linked with the D-fucosamine building block through a 1,2-α-cis-glycosidic bond, the D-glucose building block is linked with the L-fucosamine building block through a 1,2-β-trans-glycosidic bond, and the construction of the 1,2-α-cis-glycosidic bond is conducted in a mixed solvent; and the mixed solvent includes two or more of dichloromethane, diethyl ether and thiophene. According to the method of the disclosure, D-mannose is taken as a raw material, D-fucose is obtained simply, conveniently and efficiently, depending on suitable mixed solvents, the uniform construction of a cis-glycosidic bond of the D-fucose is achieved, the stereoselectivity can be up to 100%, and a very good application prospect in the aspects of the development of novel medicines and vaccines against Pseudomonas aeruginosa and the like is achieved.
专利号:US-6753347-B2 优先权日:1999-06-28 标题:Intermediates for the synthesis of benzimidazole derivatives and a process for the preparation thereof 发明人:KISHI NAOYUKI; NAKAMURA YOSHITAKA; ABE NARUMI; TAKEBAYASHI TOYONORI 权利人:SANKYO CO 摘要:This invention provides a process for the preparation of a benzimidazole derivative (I) or a pharmaceutically acceptable salt thereof, n wherein R 1 is C 1 -C 6 alkyl, C 1 -C 6 alkoxyl, etc., R 2 is C 1 -C 6 alkyl, and R 3 is hydrogen or a protecting group, which exhibits excellent hyopoglycemic action, said process comprising condensation of an amine derivative (III) with a carboxylic acid derivatives (II) to afford a compound (IV), followed by cyclization of compound (IV) in the presence of an acid.
专利号:WO-2024159724-A1 优先权日:2023-02-03 标 题:O-biphenyl oxazoline compound and synthesis method therefor 发明人:ZHU JIANSHE; WANG MINGCHUN; LI QINGYI 权利人:KEYLAB JIANGSU TECH CO LTD 摘要:A synthesis method for an o-biphenyl oxazoline compound. An aryl metal compound as represent by formula II reacts with aryl oxazoline as represented by formula III to generate the o-biphenyl oxazoline compound as represented by formula I. The o-biphenyl oxazoline compound can be used for industrial preparation of o-aminobiphenyl compounds, and used for synthesizing succinate dehydrogenase inhibitor fungicides (IV) such as fluxapyroxad, bixafen, boscalid, and pyraziflumid.
专利号:US-2003199580-A1 优先权日:1999-06-28 标 题:Intermediates for the synthesis of benzimidazole derivatives and a process for the preparation thereof