CAS: 2243-58-5; Naphthalen-2-Ylhydrazine Hydrochloride

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📜2-萘胺置于盐酸,Tin(Ll) Chloride,Sodium Nitrite体系中,化学反应生成2-萘肼盐酸盐
参考文献:使用信息地址概念设计拟肽δ类阿片受体拮抗剂.
标题:使用信息地址概念设计拟肽δ类阿片受体拮抗剂.
摘要:使用消息地址概念已经开发出具有有效的δ阿片受体拮抗剂活性的高选择性非肽配体.这种方法设想了δ阿片受体包含两个主要的识别亚位点.一个识别该药效基团的消息子位点,和一个针对δ受体类型独特并赋予选择性的地址子位点.假定δ选择性脑啡肽的消息和地址成分分别为tyr1和phe4,其中gly2-Gly3充当间隔基.这项研究中目标化合物的信息成分来自纳曲酮和相关结构.将吲哚系统与纳曲酮的c环稠合,以模拟地址成分.吲哚的苯部分被视为δ地址成分,模仿了phe4的苯基,吡咯部分用作刚性间隔物.评价了该系列的成员(1-23)对豚鼠回肠(gpi)和小鼠输精管(mvd)制剂的阿片类拮抗剂活性.Naltrindole(nti,1)是该系列中最有效的成员,δ受体的ke值约为0.1 Nm.Nti的拮抗作用比δ和μ和κ阿片受体高约220倍和350倍.Nti和该系列的选定成员与豚鼠脑膜的结合在质量上与其在mvd和gpi中的药理
Doi:10.1021/jm00168A028

专利信息

专利号:US-9035070-B2
优先权日:2010-07-30
标 题 :Process for the preparation of 1-aryl-pyrazol-3-one intermediates useful in the synthesis of sigma receptors inhibitors
发明人：BARTRA SANMARTI MARTÃ?; BERENGUER MAIMO RAMON; MEDRANO RUPEREZ JORGE; GARCIA GOMEZ JORGE; ARIZA PIQUER JAVIER
权利人:BARTRA SANMARTI MARTÃ?; BERENGUER MAIMO RAMON; MEDRANO RUPEREZ JORGE; GARCIA GOMEZ JORGE; ARIZA PIQUER JAVIER; ESTEVE QUÃ?MICA S A
摘要:The invention relates to a process for preparing 1-aryl-pyrazol-3-one intermediates, tautomers, and salts thereof, to novel intermediates, and to the use of the intermediates in the preparation of sigma receptor inhibitors.

专利号:US-2013184472-A1
优先权日:2010-07-30
标题 :Process for the Preparation of 1-ARYL-PYRAZOL-3-ONE Intermediates Useful in the Synthesis of SIGMA Receptors Inhibitors

专利号:CN-107417690-B
优先权日:2017-09-07
标 题:A kind of method for asymmetric catalytic synthesis of pyrrole indoline

专利号:CA-2800750-A1
优先权日:2010-07-30
标题 :Process for the preparation of 1-aryl-pyrazol-3-one intermediates useful in the synthesis of sigma receptors inhibitors

专利号:WO-2012013755-A1
优先权日:2010-07-30
标题:Process for the preparation of 1-aryl-pyrazol-3-one intermediates useful in the synthesis of sigma receptors inhibitors

专利号:EP-2598469-B1
优先权日:2010-07-30
标题 :Process for the preparation of 1-aryl-pyrazol-3-one intermediates useful in the synthesis of sigma receptors inhibitors