专利号:US-5786515-A 优先权日:1995-09-15 标题 :Synthesis of α-chloro or fluoro ketones 发明人:DOLLING ULF H; FREY LISA F; TILLYER RICHARD D; TSCHAEN DAVID M 权利人:MERCK & CO INC 摘要:A simple, high yielding synthesis of a-chloro ketones is described, involving acylation of Grignard and organolithium reagents with N-methoxy-N-methylchloroacetamide. The efficiency of the process is further enhanced by recycling N,O-dimethylhydroxylamine.
专利号:US-2023391818-A1 优先权日:2020-11-05 标 题:Peptide synthesis method for suppressing defect caused by diketopiperazine formation 发明人:NOMURA KENICHI; KAGE MIRAI; TAMIYA MINORU; KANAZAWA JUNICHIRO 权利人:CHUGAI PHARMACEUTICAL CO LTD 摘要:Solid-phase synthesis of a peptide has a problem that a desired elongation reaction is prevented from proceeding by diketopiperazine and a 6-membered diamine skeleton compound formed when a protective group at the N-terminal is removed. The present inventors have found that when in production of a peptide by a solid-phase method, a peptide in which an amino group at the N-terminal is protected with a protective group having an Fmoc skeleton is treated in a specific solvent with a base having a pKa of 23 or more in acetonitrile as a conjugate acid, and a peptide chain is then elongated, it is possible to solve the problem described above.
专利号:US-10899695-B2 优先权日:2017-02-06 标 题 :Process for the synthesis of 1-aryl-1-trifluoromethylcyclopropanes 发明人:MCLAREN LEE; TO DANIEL; TOVELL DAVID; ABELE STEFAN 权利人:IDORSIA PHARMACEUTICALS LTD 摘要:The present invention relates to a process for the manufacturing of 1-aryl-1-trifluoromethylcyclopropanes, which serve as intermediates for the manufacturing of calcium T channel blockers of the general formula (A) n nwhich are described in WO 2015/186056.
专利号:US-2021114953-A1 优先权日:2018-06-08 标 题:Synthesis of e,e-farnesol, farnesyl acetate and squalene from farnesene via farnesyl chloride 发明人:FISHER KARL JOSEPH; WOOLARD FRANK XAVIER 权利人:AMYRIS INC 摘要:The present disclosure provides methods for preparing polyunsaturated hydrocarbons, such as E,E-farnesol, farnesyl acetate and squalene, by base catalyzed addition of a dialkylamine to a 3-methylene-1-alkene, such as farnesene. The present disclosure also provides compositions including one more farnesene derivatives prepared using the disclosed methods.
专利号:US-3974150-A 优先权日:1972-07-21 标 题 :7β-Isocyano cephalosporin esters and process of preparation 发明人:COOK MARTIN CHRISTOPHER; LAUNDON BRIAN 权利人:GLAXO LAB LTD 摘要:Novel 6β-isocyano penicillin and 7β-isocyano cephalosporin esters of value as intermediates in the synthesis of penicillin and cephalosporin antibiotics are provided. The novel compounds may be prepared by reaction of the corresponding 6β-formamido penicillin ester or 7β-formamido cephalosporin ester with an acid halide derived from phosphorus, sulphur or carbon or from an oxygen acid of one of said elements, suitable halides including thionyl chloride or phosgene, or with a trivalent phosphorus compound such as triphenylphosphine and a halogenated hydrocarbon such as carbon tetrachloride. The conversion of the novel products to 6β- and 7β- (α-hydroxy) arylacetamido penicillins and cephalosporins respectively by reaction under acidic conditions with an aromatic aldehyde followed by treatment with an aqueous medium is also described.
专利号:US-5457238-A 优先权日:1994-06-30 标 题:Process for the preparation of fluoroketones 发明人:PETROV VIACHESLAV A; SMART BRUCE E 权利人:DU PONT 摘要:This invention concerns a process for the preparation of fluoroketones by the isomerization of corresponding epoxides, in the presence of an aluminum chlorofluoride catalyst. Fluorinated ketones are useful intermediates for the synthesis of various fluorinated compounds.
摘要:Lai, J.; Thomson, B. J.; Sammis, G. M., Science of Synthesis: Modern Strategies in Organofluorine Chemistry , (2024) 1, 19. 参考文献:10.1021/jo025591l 摘要:Ram Reddy MV, Rudd MT, Ramachandran PV. Study of fluorocarbonyls for the Baylis-Hillman reaction. J Org Chem. 2002 Jul 26;67(15):5382–5. doi: 10.1021/jo025591l.