📜2,5-环己二烯-1,4-二酮单肟置于盐酸,次磷酸,Sodium Nitrite体系中,用 1,4-二氧六环,水 作为反应溶剂,化学反应 20.0H,反应生成 1-氯-3,5-二甲氧基苯 参考文献:Sargent,Melvyn V.,Journal Of The Chemical Society. Perkin Transactions I,1982,P. 1095-1098 标题:Sargent,Melvyn V.,Journal Of The Chemical Society. Perkin Transactions I,1982,P. 1095-1098
专利号:US-8114993-B2 优先权日:2007-02-06 标题:Use of aryl chlorides in palladium-catalyzed C-H bond functionalization 发明人:DAUGULIS OLAFS; CHIONG HENDRICH 权利人:DAUGULIS OLAFS; CHIONG HENDRICH; UNIV HOUSTON SYSTEM 摘要:A one-step method for efficiently converting carbon-hydrogen bonds into carbon-carbon bonds using chloroarenes and palladium catalysts is disclosed. This method allows faster introduction of complex molecular entities, a process that would otherwise require many more steps. This invention is particularly relevant for the organic synthesis of complex molecules such as, but not limited to, pharmacophores.
专利号:US-6207837-B1 优先权日:1997-07-18 标题:Process for producing dibenzo[b,f]thiepine derivatives 发明人:OHTSUKA NAOMI; JINNO SHUJI; OKITA TAKAAKI 权利人:NIPPON SUISAN KAISHA LTD 摘要:Efficient synthesis of diaryl sulfide derivatives useful as intermediates for pharmaceutical compounds. Provision of a convenient process for producing large quantities of dibenzo[b,f]thiepine derivatives using such intermediates. n Halogen-substituted phenyl derivatives of the general formula (1): n (where X is a halogen atom and R 1 -R 5 is any substituent selected from among hydrogen, a lower alkyl group, a lower cycloalkyl group, an aryl group, a halogen atom, a lower alkoxyl group, an amino group, an N-lower acylamino group, a nitro group, a lower alkylthio group and a carboxyl group) are reacted with disulfide derivatives of the general formula (2): n (where R 6 -R 10 is any substituent selected from among hydrogen, a lower alkyl group, a lower cycloalkyl group, an aryl group, a halogen atom, a lower alkoxyl group, an amino group, an N-lower acylamino group, a nitro group, a lower alkylthio group and a carboxyl group) in the presence of metal catalysts to form a sulfide bond, thereby producing diaryl sulfide derivatives of the general formula (3): n (where R 1 -R 10 are the same as defined above) or salts thereof. Pharmaceutical compounds such as dibenzo[b,f]thiepine derivatives are produced from the diaryl sulfide derivatives or salts thereof by known techniques.
专利号:US-9006491-B2 优先权日:2009-10-22 标题 :Structure and method for synthesizing and using dialkyl(2,4,6- or 2,6-alkoxyphenyl)phosphine and its tetrafluoroborate 发明人:MA SHENGMING; LÜ BO; FU CHUNLING 权利人:MA SHENGMING; LÜ BO; FU CHUNLING; UNIV ZHEJIANG 摘要:The current invention relates to the structure, synthesis of dialkyl(2,4,6- or 2,6-alkoxyphenyl)phosphine or its tetrafluoroborate, as well as its applications in the palladium catalyzed carbon-chlorine bond activation for Suzuki coupling reactions and carbon-nitrogen bond formation reactions. The dialkyl(2,4,6- or 2,6-alkoxyphenyl)phosphine or its tetrafluoroborate could coordinate with the palladium catalyst to activate the inert carbon-chlorine bond highly selectively and catalyze Suzuki coupling reaction with arylboronic acid or carbon-nitrogen bond formation reaction with organic amines. The current invention uses only one step to synthesize dialkyl(2,4,6- or 2,6-alkoxyphenyl)phosphine and its tetrafluoroborate is stable in the air. Compared with known synthetic routes of ligands used in activating carbon-chlorine bonds, the method of current invention is short, easy to operate. Moreover, with this type of ligands, the Suzuki coupling products of optically active chlorolactones and arylboronic acids would maintain their configuration and optical purity.
专利号:CN-117945858-A 优先权日:2024-01-26 标题 :A synthesis method of cannabidiol, intermediate and preparation method thereof
专利号:CN-116813454-B 优先权日:2023-06-21 标 题:A kind of synthesis method of pterostilbene
专利号:CN-116813454-A 优先权日:2023-06-21 标题:A kind of synthesis method of pterostilbene
[参考文献]: Gary A Molander, Et Al. Cross-Coupling Of Cyclopropyl- And Cyclobutyltrifluoroborates With Aryl And Heteroaryl Chlorides. J Org Chem. 2008 Oct 3;73(19):7481-5.
合成参考文献
摘要:Molander, G. A.; Beaumard, F., Science of Synthesis Knowledge Updates, (2013) 3, 108. 摘要:Collings, J. C., Science of Synthesis Knowledge Updates, (2013) 4, 306. 摘要:Gleason, J. L.; Tiong, E. A., Science of Synthesis Knowledge Updates, (2010) 4, 287. 摘要:Stanforth, S. P., Science of Synthesis Knowledge Updates, (2015) 1, 181. 摘要:Suginome, M.; Ohmura, T., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 171.