Methyl 3-(Allyloxy)Benzoate置于氢氧化钾,氯化亚砜,二甲基硫,磷酸,臭氧,N,N-二甲基甲酰胺体系中,用 甲醇 作为反应溶剂,化学反应 4.75H,反应生成 苯并呋喃-6-羧酸 参考文献:Aminoalkylindoles: Structure-Activity Relationships Of Novel Cannabinoid Mimetics 标题:Aminoalkylindoles: Structure-Activity Relationships Of Novel Cannabinoid Mimetics 摘要:Aminoalkylindoles (Aais) Are A Novel Series Of Cannabinoid Receptor Ligands. In This Report We Disclose The Structural Features Of Aais Which Are Important For Binding To This Receptor As Measured By Inhibition Of Binding Of [h-3]Win 55212-2 (5). Functional Activity In The Mouse Vas Deferens Is Also Noted And Used To Distinguish Agonists From Potential Antagonists. The Key Structural Features For Potent Cannabinoid Activity In This Series Are A Bicyclic (Naphthyl) Substituent At The 3-Position,A Small (II) Substituent At The 2-Position,And An Aminoethyl (Morpholinoethyl) Substituent At The 1-Position. A 6-Bromo Analog,Win 54461 (31),Has Been Identified As A Potential Cannabinoid Receptor Antagonist. Modeling Experiments Were Done To Develop A Pharmacophore And Also To Compare Aai Structures With Those Of Classical Cannabinoids. The Fact That The Cannabinoid Aais Arose Out Of Work On A Series Of Cyclooxygenase Inhibitors Makes Sense Now That An Endogenous Cannabinoid Ligand Has Been Identified Which Is A Derivative Of Arachidonic Acid. Because Of Their Unique Structures And Physical Properties,Aais Provide Useful Tools To Study The Structure And Function Of The Cannabinoid Receptor(S). DOI:10.1021/jm00016A013
专利号:US-2009131688-A1 优先权日:2007-11-21 标 题 :Method for the synthesis of 4-benzofuran-carboxylic acid 发明人:BURGOS ALAIN; MARUANI MARTINE; PERRIN FLORENCE; FREIN STEPHANE 权利人:ZACH SYSTEM 摘要:The invention concerns a novel method for synthesis of 4-benzofuran-carboxylic acid or alkyl ester thereof. n This method is characterized in that a reaction for aromatization of a compound of formula (II) is performed for the synthesis of the compound of formula (I), according to the scheme A2 below: n n n n n n n n n n wherein R independently represents hydrogen or a linear or branched C 1 - 15 alkyl group. n With the invention, it is possible to industrially synthesize 4-benzofuran-carboxylic acid or alkyl ester thereof with good yield and very good purity.
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