环丙甲酸置于硫酸体系中,用 乙醇 作为反应溶剂,以98%的收率获得产物环丙基甲酸乙酯 参考文献:Processes For The Preparation Of Cyclopropanecarboxylic Acid And 标题:Processes For The Preparation Of Cyclopropanecarboxylic Acid And 摘要:本发明公开了一种使用分子氧作为氧化剂,通过非催化氧化环丙基甲醛制备环丙基甲酸的方法.同时,本发明还公开了从环丙基甲酸制备酰胺,酯和酸氯化物的方法.
专利号:US-9085538-B2 优先权日:2010-07-26 标题:Process for the preparation of key intermediates for the synthesis of statins or pharmaceutically acceptable salts thereof 发明人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO 权利人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO; LEK PHARMACEUTICALS 摘要:The invention relates to commercially viable process for the synthesis of key intermediates for the preparation of statins, in particular Rosuvastatin and Pitavastatin or respective pharmaceutically acceptable salts thereof. A new simple and short synthetic route for key intermediates is presented which benefits from the use of cheap and readily available starting materials, by which the conventionally most frequently used DIBAL-H as reducing agent can be avoided.
专利号:WO-9611194-A1 优先权日:1994-10-06 标题:Pyridonecarboxylic acid derivative and intermediate for the synthesis of the same 发明人:OKADA HIDETSUGU; CHIBA KATSUMI; TOMINAGA YUKIO; MINAMI AKIRA 权利人:DAINIPPON PHARMACEUTICAL CO; OKADA HIDETSUGU; CHIBA KATSUMI; TOMINAGA YUKIO; MINAMI AKIRA 摘要:A pyridonecarboxylic acid derivative represented by general formula (I), an ester and a salt thereof, an antibacterial agent containing the same, and a bicyclic amine compound serving as a direct intermediate for the synthesis of the pyridonecarboxylic acid derivative, wherein R represents cycloalkyl, optionally substituted phenyl, etc.; G represents carbon, etc.; A represents C-Z (Z being hydrogen, halogeno, lower alkoxy, etc.) or nitrogen; X represents hydrogen, amino, etc.; Y represents hydrogen or halogeno; m is an integer of 1 to 3; and W represents -(CH2)nN(R1)R2 (R1 and R2 being the same or different and each representing hydrogen, lower alkyl, etc., and n being an integer of 0 or 1).
专利号:US-6274383-B1 优先权日:1997-12-15 标题:Methods for synthesizing libraries of dihydro-quinazolinones 发明人:GAO YUN 权利人:SEPRACOR INC 摘要:Synthetic methods for solution and solid-phase synthesis of combinatorial libraries of dihydro-quinazolinones, including synthesis of 2,3-dihydro-3-alkoxy-4(1H)-quinazolinones or 2,3-dihydro-3-hydroxy-4(1H)-quinazolinones via the Lewis-acid catalyzed reaction of an appropriate 2-aminobenzamide with an aldehyde at ambient temperature performed on a solid support or in solution.
专利号:US-2018148745-A1 优先权日:2015-05-26 标题:Hemoprotein catalysts for improved enantioselective enzymatic synthesis of ticagrelor 发明人:ARNOLD FRANCIS H; RENATA HANS; MCINTOSH JOHN A; LEWIS RUSSELL D; KAN SEK BIK JENNIFER; HERNANDEZ KARI; COELHO PEDRO; ROZZELL DAVID; ZHANG CHEN 权利人:CALIFORNIA INST OF TECHN; PROVIVI INC 摘要:The present invention provides methods by which trans-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropylamine and related cyclopropane compounds are prepared using synthetic strategies that include a biocatalytic cyclopropanation step.
专利号:US-2007275962-A1 优先权日:2003-09-10 标 题:Heterobicyclic Compounds as Pharmaceutically Active Agents 发明人:KOUL ANIL; KLEBL BERT; MULLER GERHARD; MISSIO ANDREA; SCHWAB WILFRIED; HAFENBRADL DORIS; NEUMANN LARS; SOMMER MARC-NICOLA; MULLER STEFAN; HOPPE EDMUND; FREISLEBEN ACHIM; BACKES ALEXANDER; HARTUNG CHRISTIAN; FELBER BEATRICE; ZECH BIRGIT; ENGKVIST OLA; KERI GYORGY; ORFI LASZLO; BANHEGYI PETER; GREFF ZOLTAN; HORVATH ZOLTAN; VARGA ZOLTAN; MARKO PETER; PATO JANOS; SZABADKAI ISTVAN; SZEKELYHID ZSOLT; WACZEK FRIGYES 权利人:GPC BIOTECH AG 摘要:Described are heterobicyclic compounds such as 4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylic acid amides, 4,7-dihydro-5H-thieno[2,3-c]thiopyran 3-carboxylic acid amides, 4,7-dihydro-5H-thieno[2,3-c]pyran-3-carboxylic acid amides, or benzo[b]thiophene-3-carboxylic acid amides and pharmaceutically acceptable salts thereof, the use of these derivatives for the prophylaxis and/or treatment of various diseases such as infectious diseases, including mycobacteriainduced infections and opportunistic diseases, prion diseases, immunological diseases, autoimmune diseases, bipolar and clinical disorders, cardiovascular diseases, cell proliferative diseases, diabetes, inflammation, transplant rejections, erectile dysfunction, neurodegenerative diseases and stroke, as well as compositions containing at least one heterobicyclic compound and/or pharmaceutically acceptable salts thereof. Furthermore, reaction procedures for the synthesis of the heterobicyclic compound are disclosed.
专利号:US-7405310-B2 优先权日:2001-03-05 标 题:Non-nucleoside reverse transcriptase inhibitors 发明人:LINDSTROM STEFAN; SAHLBERG CHRISTER; WALLBERG HANS; KALYANOV GENAIDY; ODEN LOURDES SALVADOR; NAESLUND LOTTA 权利人:MEDIVIR AB 摘要:This invention relates to non-nucleoside reverse transcriptase inhibitors active against HIV-1 and having an improved resistance and pharmacokinetic profile. The invention further relates to novel intermediates in the synthesis of such compounds and the use of the compounds in antiviral methods and compositions.