CAS: 1986-47-6; Trans-2-Phenylcyclopropanamine Hydrochloride

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📜Methyl Trans-2-Phenylcyclopropanecarboxylate置于盐酸,Sodium Hydroxide,叠氮磷酸二苯酯,三乙胺体系中,用 甲醇 用作溶剂,化学反应 44.0H,反应生成反苯环丙胺盐酸盐
参考文献:Trans-2-Aryl-N,N-Dipropylcyclopropylamines: Synthesis And Interactions With 5-Ht1A Receptors
标题:Trans-2-Aryl-N,N-Dipropylcyclopropylamines: Synthesis And Interactions With 5-Ht1A Receptors
摘要:Twelve N,N-Dipropyl-Substituted Derivatives Of Trans-2-Arylcyclopropylamine Have Been Prepared And Assayed For Their Ability To Displace [h-3]-8-Oh-Dpat From Rat Brain 5-Ht1A Receptors. The New Derivatives Include Phenyl (7A),Bromo-(7B) And Fluorophenyl (7C-E),2-Methoxy-5-Fluorophenyl (7H),And 2-Hydroxy-5-Fluorophenyl (7I) As Well As Trifluoromethylphenyl (7F) And 2,3-Dichlorophenyl (7G) Analogues. In The Present Series Of Compounds,Electron-Withdrawing Substituents In The Phenyl Ring Appear To Decrease The Affinity For 5-Ht1A Receptors. In Contrast,Electron-Rich Aryl Groups,Such As 2-Or 3-Thienyl (7J And 7K,Respectively),Provide Compounds With High Affinity. The Additional Bulk Produced By The Aromatic Moiety In The 2-Benzothienyl Derivative 7I Appears To Be Detrimental To 5-Ht1A Receptor Affinity. The Racemic Mixtures Of The Interesting 7J And 7I Were Resolved Into The Enantiomers; 7J And 7I Exhibited A High Enantiomeric 5-Ht1A Receptor Affinity Ratio (75-Fold And 100-Fold,Respectively). The Enantiomers Of 7J And 7I Were Evaluated In Vivo By Use Of Biochemical And Behavioral Tests In Rats. Compound (Lr,2R)-7J Behaved As A Partial Agonist Whereas (1R,2S)-7I Appeared As An Efficacious 5-Ht1A Receptor Agonist,Stimulating Both Autoreceptors And Postsynaptic Receptors.
Doi:10.1021/jm9507136

专利信息

专利号:US-7109377-B2
优先权日:1996-10-16
标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products
发明人：SCHREIBER STUART L; SHAIR MATTHEW D; TAN DEREK S; FOLEY MICHAEL A; STOCKWELL BRENT R
权利人:HARVARD COLLEGE
摘要:The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.

专利号:US-2003082830-A1
优先权日:1996-10-16
标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products

专利号:US-7468375-B2
优先权日:2004-04-26
标题:Inhibitors of the HIV integrase enzyme
发明人：DRESS KLAUS RUPRECHT; HU QIYUE; JOHNSON TED WILLIAM; PLEWE MICHAEL BRUNO; TANIS STEVEN PAUL; WANG HAI; YANG ANLE; YIN CHUNFENG; ZHANG JUNHU
权利人:PFIZER
摘要:The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as modulators or inhibitors of the human immunodeficiency virus (“HIVâ€?) integrase enzyme.

专利号:WO-0006525-A9
优先权日:1998-07-25
标题:Synthesis of combinatorial libraries of compounds reminiscent of natural products

专利号:WO-0006525-A2
优先权日:1998-07-25
标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products

专利号:US-6448443-B1
优先权日:1996-10-16
标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products