专利号:US-2006167025-A1 优先权日:2004-12-22 标 题:Tricyclic amino alcohols, processes for synthesis of same and use of same as anti-inflammatory drugs 发明人:BERGER MARKUS; SCHMEES NORBERT; SCHAECKE HEIKE; BAURLE STEFAN; REHWINKEL HARTMUT; MENGEL ANNE; KROLIKIEWICZ KONRAD; GROSSBACH DANJA; VOIGTLAENDER DAVID 权利人:BERGER MARKUS; SCHMEES NORBERT; SCHAECKE HEIKE; BAURLE STEFAN; REHWINKEL HARTMUT; MENGEL ANNE; KROLIKIEWICZ KONRAD; GROSSBACH DANJA; VOIGTLAENDER DAVID 摘要:The invention relates to tricyclic amino alcohols of general formula (I) n nmethod for synthesis of same and use of same as anti-inflammatory agents.
专利号:US-4374979-A 优先权日:1981-04-27 标 题:Regiospecific synthesis of anthracyclinone compounds such as daunomycinone 发明人:MITSCHER LESTER A 权利人:UNIV KANSAS ENDOWMENT ASS 摘要:A regiospecific synthesis for anthracyclinones asymmetric is disclosed. The synthesis is based upon a regiospecific bromination of the C-7 position of the alpha -tetralone which after transposing the keto group to the beta -position and reaction with an organo-lithium compound is condensed with a phthalate ester.
专利号:US-7884243-B2 优先权日:2003-12-22 标 题:Process for the synthesis of eneamide derivatives 发明人:BURGOS ALAIN; BERTRAND BLANDINE; ROUSSIASSE SONIA; PLUVIE JEAN-FRANCOIS; BLANCHET SYLVIE; MARTIN JULIETTE; PERRIN FLORENCE; BOURDEAU FRANCOISE 权利人:ZACH SYSTEM 摘要:A process for the production of ene-amide derivatives represented by the formula (I) n nwherein R1 and R2 and R3 are independently a hydrogen atom, an alkyl, a cycloalkyl, a cycloalkylalkyl, an alkylaryl, an aryl, a heterocycle, a cyano, an alkoxy, an aryloxy, a carboxyl, a carbamoyl, —CONR5R6 (in which R5 and R6 are independently an alkyl, arylalkyl or aryl group said ring being substituted or not with a functional group or with R5) or —COOR5 group (in which R5 is an alkyl, alkylaryl or aryl group), said alkyl, cycloalkyl, cycloalkylalkyl, alkylaryl and aryl groups being substituted or not with a functional group or with R5; or R1 and R2 taken together, may form a ring (which terms includes mono-, di- and higher polycyclic ring systems); R4 is a hydrogen atom, an alkyl, an aryl, an alkylaryl, said groups are substituted or not with a halogen atom as Cl, Br, or F; X is an oxygen atom or a leaving group and m is an integer 1 or 2; when m is 1 then X is a leaving group; when m is 2 then X is a oxygen atom, which comprise: a hydrogenation/isomerization reaction in presence of a heterogeneous catalyst, of an oxime derivatives of formula (II)n n nwherein R1, R2 and R3 are as defined above with an acyl derivative of formula (III) (R4CO) m X wherein R4, m and X are as defined above.
专利号:EP-0684234-B1 优先权日:1994-05-26 标 题:Synthesis of benzoquinolinones 发明人:AUDIA JAMES EDMUND; DROSTE JAMES JOSEPH; HEATH PERRY CLARK; WEIGEL LELAND OTTO 权利人:LILLY CO ELI 摘要:A process for preparing 10b-methyl-3-oxo-benzo[f] quinolines of the formula wherein R is hydrogen, methylthio, chloro, bromo or fluoro, and is located at the 7-, 8- or 9-position; comprising reacting a compound of the formula with methyl iodide in an ether solvent to prepare a compound of the formula combining acrylic anhydride or acryloyl chloride with the reaction mixture comprising the compound of formula III to prepare a compound of the formula quenching the reaction with sodium bicarbonate, evaporating the organic solution comprising the compound of formula IV; and combining the residue comprising the compound of formula IV with a trialkylsilane and trifluoroacetic acid in the absence of a solvent to prepare the compound of formula I.
专利号:US-7557237-B2 优先权日:2003-09-09 标题:Process for the synthesis of 3-(3-fluoro-4-hydroxyphenyl)-7-hydroxynaphthonitrile 发明人:WU YANZHONG; REN JIANXIN; GHOSH MOUSUMI; LEVENT MAHMUT; SUTHERLAND KAREN W; RAVEENDRANATH PANOLIL 权利人:WYETH CORP 摘要:A process for making a compound of formula I n nand intermediate compounds thereof, wherein R 1 is CN, F or Cl; R 2 is H or Br; and R 3 and R 4 are each independently H or F. The compounds of formula I are useful in the treatment of chronic inflammatory diseases, such as rheumatoid arthritis.
专利号:US-3697597-A 优先权日:1968-09-21 标 题:Process for the preparation of alpha-oximinoalkyl ketones 发明人:DORLARS ALFONS 权利人:BAYER AG 摘要:Alpha -Oximino ketones, for example, oximinodipropyl ketone, are prepared by reacting a ketone in an inert organic solvent immiscible with water in the presence of a hydrogen halide with an amount of alkyl nitrite that is insufficient for complete nitrosation followed by extracting the ketone formed with an aqueous alkali solution, removing the alkaline extract formed and isolating the Alpha -oximino ketone. The ketones formed are useful as intermediates in the synthesis of pharmaceutical compounds, dyes, analytical reagents, plant protection agents, and optical brighteners.
[参考文献]: Barry M Trost, Et Al. Palladium-Catalyzed Asymmetric Allylic Alkylation Of Alpha-Aryl Ketones. Angew Chem Int Ed Engl. 2002 Sep 16;41(18):3492-5. [参考文献]: M Goto, Et Al. Rate Enhancement With High Ratio Of The Monoalkylated Product To The Dialkylated Product In The Alkylation Of The Lithium Enolate Of 1-Tetralone With Reactive Alkyl Halides. Chem Pharm Bull (Tokyo). 2000 Oct;48(10):1529-31. [参考文献]: R D Mattes, Et Al. Ethanol Perception And Ingestion. Physiol Behav. 2001 Jan;72(1-2):217-29.
合成参考文献
摘要:Petasis, N. A., Science of Synthesis, (2010) 47, 183. 摘要:Petasis, N. A., Science of Synthesis, (2010) 47, 236. 摘要:Petasis, N. A., Science of Synthesis, (2010) 47, 238. 摘要:Petasis, N. A., Science of Synthesis, (2010) 47, 168. 摘要:Petasis, N. A., Science of Synthesis, (2010) 47, 224.