📜对硝基苯乙酸乙酯 在 镍 盐酸,Sodium Hydroxide,氢气体系中,20.0~130.0 °C,17.29 Mpa 条件下,反应 66.5H,获得 Ethyl 2-((1R,4R)-4-Aminoyclohexyl)Acetate hydroChloride
参考文献:Aminopyrimidines With High Affinity For Both Serotonin And Dopamine Receptors
标题:Aminopyrimidines With High Affinity For Both Serotonin And Dopamine Receptors
摘要:A Series Of {4-[2-(4-Arylpiperazin-1-yl)Alkyl]Cyclohexyl}Pyrimidin-2-Ylamines Was Prepared And Found To Have Receptor Binding Affinity For D2 And D3 Dopamine (Da) Receptors And Serotonin 5-Ht1A Receptors. The Structural Contributions To D2/D3 And 5-Ht1A Receptor Binding Of The Aminopyrimidine,Cycloalkyl,And Phenylpiperazine Portions Of The Molecule Were Examined. From These Studies Compounds 14,39,42,43,Having Potent Affinity For Both Da D2 And 5-Ht1A Receptors,Were Evaluated For Intrinsic Activity At These Receptors,In Vitro And In Vivo. Compound 14 (Pd 158771) Had A Profile Indicative Of Partial Agonist Activity At Both D2 And 5-Ht1A Receptors Causing Partially Decreased Synthesis Of The Neurotransmitters Da And 5-Ht And Their Metabolites. This Compound Has A Profile In Behavioral Tests That Is Predictive Of Antipsychotic Activity,Suggesting That Mixed,Partial Agonists Such As 14 May Have Utility As Antipsychotic Agents With Increased Efficacy And Decreased Side Effects.
Doi:10.1021/Jm9707378