对甲氧基苯乙酸置于氯化亚砜体系中,用95%的收率获得产物4-甲氧基苯乙酰氯 参考文献:Synthesis,Selective Aldose Reductase Inhibitory Profile And Antihyperglycaemic Potential Of Certain Parabanic Acid Derivatives 标题:Synthesis,Selective Aldose Reductase Inhibitory Profile And Antihyperglycaemic Potential Of Certain Parabanic Acid Derivatives 摘要:描述了某些对二氨基甲酸衍生物1A-P的合成和醛糖还原酶抑制剖面.此外,研究了这些化合物的抗高血糖潜力.在这个系列中,最活跃的抑制剂是化合物1G,1P和10,它们在浓度为1 X 10−4时分别显示出36.6%,90%和91%的抑制活性.它们的ic50分别为2 X 10−6,7.5 X 10-8和5 X 10-8.化合物10表现出明显的抗高血糖效果. DOI:10.3797/scipharm.Aut-01-204
专利号:US-2008045726-A1 优先权日:2004-05-10 标题 :Spirolactams and Their Synthesis 发明人:NOHEDA MARIN PEDRO; BERNABE PAJARES MANUEL; MAROTO QUINTANA SERGIO; TABARES CANTERO NURIA 权利人:ESTEVE LABOR DR 摘要:New spirolactams of formula (I) having a cycloexadienone moiety which are highly stable due to pi interactions between the W group and the dienone moiety. They are useful as UV absorbers and as intermediates for the synthesis of active biomolecules.
专利号:US-6413957-B1 优先权日:1998-04-21 标题:Methods of inhibiting cell proliferation using indeno [1,2-c]pyrazol-4-ones 发明人:NUGIEL DAVID A; CARINI DAVID J; DI MEO SUSAN V; YUE EDDY W 权利人:BRISTOL MYERS SUIBB PHARMA COM 摘要:The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): n that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits know as cyclins A-G. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.
专利号:US-2008281094-A1 优先权日:2004-05-10 标题 :Regioselective Functionalisation and Protection of Spirolactams 发明人:NOHEDA MARIN PEDRO; PAJARES MANUEL BERNABE; QUINTANA SERGIO MAROTO; CANTERO NURIA TABARES; ARENAS RAUL BENITO 权利人:ESTEVE LABOR DR 摘要:The invention provides highly functionalised spiro-fused lactams of en formula (I) having a cyclohexane moiety with the desired number of protected or un-protected functional groups or carbonated structures, which are introduced with high stereo and regioselectivity, as well as processes for their obtention. These compounds are useful for the synthesis of abroad range of bioactive molecules, such as condoritols and aminoinositols and their analogues.
专利号:US-8481501-B2 优先权日:2004-05-28 标 题 :Synthesis of metabolically stable analgesics, pain medications and other agents 发明人:CASHMAN JOHN R; MACDOUGALL JAMES M 权利人:CASHMAN JOHN R; MACDOUGALL JAMES M; HUMAN BIOMOLECULAR RES INST 摘要:Disclosed are analgesic-related compositions and methods of using the compositions for modulation of analgesic receptor activity. The compositions and methods are useful for reducing pain, as well as for therapeutic intervention of addictions or other diseases or disorders amenable to treatment or prophylaxis by modulation of analgesic receptor signaling.
专利号:US-7291728-B2 优先权日:2004-05-10 标题:Spirolactams and their synthesis 发明人:MARIN PEDRO NOHEDA; PAJARES MANUEL BERNABE; QUINTANA SERGIO MAROTO; CANTERO NURIA TABARES 权利人:ESTEVE LABOR DR 摘要:The present invention is directed to a compound of formula I: n nwherein R 1 and R 2 are independently selected from H, halogen, protected or unprotected hydroxy, alkylsilyloxy, substituted or unsubstituted alkyl or cycloalkyl, substituted or unsubstituted alkoxy or aryloxy, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, nitro, amino, mercapto or alkylthio;n R 3 and R 4 are independently selected from H, substituted alkyl, substituted or unsubstituted alkoxy or aryloxy, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl; Z is —(CRaRb) n — wherein n is a number selected from 1, 2, 3 and Ra and Rb are each independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryloxy, substituted or unsubstituted amino or halogen; Y is selected from —O—, —S—, —N(Ra)— or —C(O)—, wherein Ra is as previously defined and does not form a cyclic ring; W is a group with sufficient electronic density to stabilize the compound through Ï€ interactions with the benzodienone moiety; or a salt thereof. n The present invention also provides a method for its synthesis and intermediates thereof, as well as a method for absorbing UV comprising exposing a compound of formula I to UV radiation.
专利号:US-7250435-B2 优先权日:1999-10-20 标 题:Acylsemicarbazides as cyclin dependent kinase inhibitors useful as anti-cancer and anti-proliferative agents 发明人:NUGIEL DAVID A; CARINI DAVID J; DI MEO SUSAN V; VIDWANS ANUP P; YUE EDDY 权利人:BRISTOL MYERS SQUIBB PHARMA CO 摘要:The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): n nthat are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits know as cyclins A-G.n n This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.
参考标题:Directed Remote Lateral Metalation: Highly Substituted 2-Naphthols And Binols By In Situ Generation Of A Directing Group 作者:Jignesh J. Patel,Marju Laars,Wei Gan,Johnathan Board,Matthew O. Kitching,Victor Snieckus |发布日期:2018.7.20 摘要:General Synthesis Of Highly Substituted 2‐naphthols Based On A New Carbanionic Reaction Sequence Is Demonstrated. The Reaction Exploits The Dual Nature Of Lithium Bases Consisting Of Consecutive Ring Opening Of Readily Available Coumarins With Either Linet2 Or Linipr2 Into Z‐cinnamamides, Thus Generating A Directing Group In Situ And Allowing, By Conformational Freedom, A Lateral Directed Remote Metalation
合成参考文献
摘要:Champagne, P. A.; Drouin, M.; Paquin, J.-F., Science of Synthesis Knowledge Updates, (2016) 1, 419. 摘要:Gouverneur, V.; Lozano, O., Science of Synthesis: Stereoselective Synthesis, (2011) 3, 887. 摘要:Ishihara, K.; Sakakura, A., Science of Synthesis: Stereoselective Synthesis, (2011) 3, 110.