5-羟基-2-戊酮 反应生成 环丙甲基酮 参考文献:Rakhimkulov,A. G.; Kolesnikov,I. M.; Poteryakhin,V. A.,Journal Of Applied Chemistry Of The Ussr,1982,Vol. 55,# 8,P. 1752-1754 标题:Rakhimkulov,A. G.; Kolesnikov,I. M.; Poteryakhin,V. A.,Journal Of Applied Chemistry Of The Ussr,1982,Vol. 55,# 8,P. 1752-1754
专利号:US-11926589-B2 优先权日:2019-07-09 标 题 :Process for the synthesis of non-racemic cyclohexenes 发明人:REISMAN SARAH; ROMBOLA MICHAEL; LADD CAROLYN L; MCLAUGHLIN MARTIN JOHN; ZUEND STEPHAN; GOETZ ROLAND 权利人:BASF CORP; CALIFORNIA INST OF TECHN 摘要:This invention relates to a process for the synthesis of a non-racemic cyclohexene compound of formula (I) by a Diels-Alder reaction of a compound of formula (II) with a compound of formula (III) wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 and Y have the meanings as defined in the description in the presence of a catalyst comprising at least one m-valent metal cation M m+ wherein the metal M is selected from Scandium (Sc), Yttrium (Y), Lanthanum (La), Cerium (Ce), Praseodymium (Pr), Neodymium (Nd), Promethium (Pm), Samarium (Sm), Europium (Eu), Gadolinium 15 (Gd), Terbium (Tb), Dysprosium (Dy), Holmium (Ho), Erbium (Er), Thulium (Tm), Ytterbium (Yb), Lutetium (Lu), Gallium (Ga) and Indium (In), and m is an integer of 1, 2 or 3, and a chiral ligand of the formula (IV) wherein R 10a , R 10b , R 10c , R 10d , R 10a′ , R 10b′ , R 10c′ , R 10d′ , Z and Z′ have the meanings as defined in the description.
专利号:US-11708363-B2 优先权日:2020-09-30 标 题:Method for preparing a key intermediate for the synthesis of statins 发明人:CHEN FENER; CHENG DANG; LIU MINJIE; HUANG ZEDU; TAO YUAN; WANG JIAQI 权利人:UNIV FUDAN 摘要:Disclosed herein relates to organic synthesis, and more particularly to a method for preparing a key intermediate for the synthesis of statins. The key intermediate is 2-[(4R,6S)-6-[(benzo[d]thiazol-2-ylthio)methyl]-2,2-disubstituted-1,3-dioxan-4-yl] acetate of formula (I): n nwhere R 1 is a C 1 -C 8 alkyl group, a C 3 -C 8 cycloalkyl group, a monosubstituted or polysubstituted aryl group, or monosubstituted or polysubstituted aralkyl group; R 2 is hydrogen, or monosubstituted or polysubstituted C 1 -C 3 alkyl group, or halogen; and R 3 and R 4 are each independently a C 1 -C 5 alkyl group, a C 3 -C 7 cycloalkyl group, a C 3 -C 7 cycloalkenyl group, a C 1 -C 3 alkoxy group, a C 6 -C 10 aryl group, or C 7 -C 12 aralkyl group. In the method, a halomethyl compound and a thiol reagent are subjected to nucleophilic substitution in an organic solvent to synthesize a thioether, which then undergoes ketal exchange reaction with a carbonyl compound (V) in the presence of an organic acid to obtain a target product.
专利号:US-6028237-A 优先权日:1996-12-16 标题:Synthesis of cyclopropylacetylene 发明人:PARSONS JR RODNEY LAWRENCE 权利人:DU PONT PHARM CO 摘要:The present invention relates generally to novel methods for the synthesis of cyclopropylacetylene which is a reagent in the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one which is a useful human immunodeficiency virus (HIV) reverse transcriptase inhibitor.
专利号:US-9994508-B2 优先权日:2012-12-11 标 题:Versatile and functionalised intermediates for the synthesis of vitamin D and novel vitamin D derivatives 发明人:LOPEZ PEREZ BORJA; SIGUEIRO PONTE RITA; MAESTRO SAAVEDRA MIGUEL A; MOURINO MOSQUERA ANTONIO 权利人:ENDOTHERM GMBH 摘要:Novel intermediates for the complete synthesis of vitamin D are provided that allow a great versatility of functional groups in the final vitamin derivatives. Vitamin derivatives that are epimeric in position 3 and vitamin derivatives with a wide range of functionalities in position 18, including compounds with isotopic labelling are provided.
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-2022127640-A1 优先权日:2020-12-16 标题:Process for synthesis of furan-based diamines 发明人:GUO RUIJING; PIRES RAUL; BEUCK SASKIA; LATORRE MARTINEZ IRENE CRISTINA; PAN XIANGCHENG; JIANG YUAN 权利人:COVESTRO DEUTSCHLAND AG; GUO RUIJING 摘要:The invention provides a process for the synthesis of furan-based diamines based on renewable resources.
[参考文献]: Shigeo Hayashi, Et Al. Design, Synthesis And Structure-Activity Relationship Studies Of Novel And Diverse Cyclooxygenase-2 Inhibitors As Anti-Inflammatory Drugs. J Enzyme Inhib Med Chem. 2014 Dec;29(6):846-67.
合成参考文献
摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 51. 摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 146. 摘要:Gao, W.-C.; Tian, J., Science of Synthesis Knowledge Updates, (2020) 3, 250. 摘要:Zhang, J., Science of Synthesis Knowledge Updates, (2010) 4, 244. 摘要:Heydt, H., Science of Synthesis Knowledge Updates, (2014) 3, 409.