专利号:US-7276637-B2 优先权日:2002-08-02 标题:Synthesis of cyclohexanone derivatives 发明人:BRANDS KAREL MARIE JOSEPH; DAVIES ANTONY JOHN; OAKLEY PAUL JOSEPH; SCOTT JEREMY PETER; SHAW DUNCAN EDWARD; TEALL MARTIN RICHARD 权利人:MERCK & CO INC 摘要:A novel process for preparing cyclohexanone derivatives of formula (I) n nis described. The products are useful as gamma secretase inhibitors, or as intermediates in the synthesis of other gamma secretase inhibitors.
专利号:US-6177572-B1 优先权日:1997-08-20 标题 :Solid and liquid-phase synthesis of benzoxazoles and benzothiazoles and their use 发明人:WANG FENGJIANG 权利人:SEPRACOR INC 摘要:Methods for preparing benzoxazoles and benzothiazoles on solid supports. Substituted benzothiazoles and benzoxazoles, libraries of the compounds, and methods of using the compounds are also disclosed.
专利号:US-4661626-A 优先权日:1985-03-11 标题 :Process for the production of 2-isocyanato-2,3-dehydrocarboxylic acid esters 发明人:EFFENBERGER FRANZ; KUEHLWEIN JUERGEN; DRAUZ KARLHEINZ 权利人:DEGUSSA 摘要:There are produced 2-isocyanato-2,3-dehydrocarboxylic acid esters of the general formula: (I) in which R1 is a straight chain or branched C1-C4-alkyl group, a phenyl group or a benzyl group, R2 is hydrogen or a methyl group and R3 is hydrogen, a straight chain or branched C1-C16-alkyl group, a C3-C8-cycloalkyl group, a C1-C6-alkylmercapto group or a phenyl group by reacting a 2-azido-carboxylic acid ester of the general formula: (II) in an inert solvent at a temperature between 0 DEG and 150 DEG C. with phosgene or diphosgene in the presence of a perrhenate. The compounds of general formula (I) can be converted into the corresponding Z- or BOC-protected 2,3-dehydro-2-amino-carboxylic acid ester with benzyl alcohol or with tert. butyl alcohol, which esters in turn are valuable building blocks for the synthesis of dehydropeptides.
专利号:US-7411088-B2 优先权日:2004-02-20 标 题:Stereoselective synthesis of a 4,4-disubstituted cyclohexanepropanoic acid 发明人:BRANDS KAREL MARIE JOSEPH; BREWER SARAH ELIZABETH; DAVIES ANTONY JOHN; DOLLING ULF H; HAMMOND DEBORAH CAMILLE; LIEBERMAN DAVID ROSS; SCOTT JEREMY PETER 权利人:MERCK & CO INC; MERCK SHARP & DOHME 摘要:There is provided stereoselective route to a compound of formula I: n nwherein R represents H or an alkali metal, Ar 1 represents 4-chlorophenyl and Ar 2 represents 2,5-difluorophenyl.
专利号:US-3962217-A 优先权日:1969-10-24 标 题 :Process for the manufacture of Δ16 -steroid-14β,18,20-triols and -14β,20-diol-18-ols of the pregnane series 发明人:WEHRLI HANSULI; JEGER OSKAR 权利人:CIBA GEIGY CORP 摘要:The invention is for a selective reduction of the 20- oxo group in Δ 16 -steroid-14β,18-diol-20-ones of the pregnane series to form the two epimeric 20-alcohols having the 20 S and 20 R configuration. The process is especially intended for the manufacture of alkaloids of the batrachotoxin type, particularly for batrachotoxinine A, which is a pregnane derivative having a 20 S alcohol grouping, and epimers and derivatives, such as epi-batrachotixinine A or 7,8-dihydrobatrachotoxinine A. The process is characterized by reducing the said Δ 16 -steroid-14β,18-diol-20-ones in form of their 14,18-ketals, for instance the 14,18 acetonides and using appropriate complex light metal hydrides and operating at appropriate temperatures. The separation of the two isomers is easy and can be effected by the usual physical operations, such as crystallization or chromatography. In the 14β,18,20-triols obtained the 18-hydroxy group can be dehydrogenated to the corresponding 18-aldehydes, which are intermediates necessary in the synthesis of the said pharmacological interesting substances, such as batrachotoxin, by treatment with a sulphoxide in the presence of a carboxylic acid anhydride.
专利号:US-6664282-B2 优先权日:1999-09-17 标 题:Synthesis of [3,5,7]-1H-imidazo [1,5-a]imidazol-2 (3H)- one compounds 发明人:ELABDELLAOUI HASSAN M; OSTRESH JOHN M; HOUGHTEN RICHARD A 权利人:TORREY PINES INST 摘要:Individual substituted [3,5,7]-1H-imidazo[1,5-a]imidazol-2(3H)-one compounds and their pharmaceutically-acceptable salts are disclosed, as are libraries of such compounds. Methods of preparing and using the libraries of compounds as well as individual compounds of the libraries are also disclosed.
摘要:Saleh, B. A.; Elliott, M. C., Science of Synthesis Knowledge Updates, (2015) 2, 402. 摘要:Jie, X.; Su, W., Science of Synthesis, (2022) , 27. 摘要:Leclerc, E., Science of Synthesis: Knowledge Updates, (2024) 3, 240.