2-(Trans-4-Hydroxycyclohexyl)Isoindoline-1,3-Dione置于盐酸,溴,Pyridinium Chlorochromate体系中,用 1,4-二氧六环,二氯甲烷,水,溶剂黄146,N,N-二甲基甲酰胺 用作溶剂,化学反应 7.5H,反应生成4,5,6,7-四氢-2,6-苯并噻唑二胺 参考文献:一系列新的氨基甲酰基胍的药理学表征表明在h 2 R和d 3 R处有强烈的激动作用 标题:一系列新的氨基甲酰基胍的药理学表征表明在h 2 R和d 3 R处有强烈的激动作用 摘要:即使在今天,组胺h 2受体(h 2 R)在中枢神经系统(cns)中的作用仍然广为人知.在先前的研究中,许多二聚体,高亲和力和亚型选择性的氨基甲酰基胍型配体,例如ur-Nk22(5,P K I = 8.07)被报道为h 2 R激动剂.但是,它们在中枢神经系统中研究h 2 R的适用性因其分子和药代动力学特性(例如高分子量)而受到限制,因此其生物利用度有限.满足对更多类似毒品的h 2的需求r激动剂具有高亲和力,我们合成了一系列含有各种间隔基和侧链部分的单体(硫代)氨基甲酰基胍型配体.这种结构上的简化导致了有效的(部分)激动剂(豚鼠右心房,[ 35 S]Gtpγs和β-Arrestin2募集试验),其人类(h)h 2 R亲和力在一位纳摩尔范围内(p K I(139,Ur-Kat523):8.35; P K I(157,Ur-Mb-69):8.69).本文介绍的大多数化合物对hh 2 R表现出出色 Doi:10.1016/j.Ejmech.2021.113190
专利信息
专利号:US-9512096-B2 优先权日:2011-12-22 标题 :Synthesis of amine substituted 4,5,6,7-tetrahydrobenzothiazole compounds 发明人:CHEN WEIRONG; HUMORA MICHAEL; KWOK DAW-LONG ALBERT; KIESMAN WILLIAM F; IRDAM ERWIN AYANDRA 权利人:KNOPP BIOSCIENCES LLC; KNOPP BIOSCIENCES LLP 摘要:The present invention is related to an improved process for the preparation of amino-substituted 4,5,6,7-tetrahydrobenzothiazole compounds of formula I, such as the compound 2-amino-4,5,6,7-tetrahydro-6-(n-propylamino)benzothiazole. The invention further relates to an improved synthesis of (R)-2-amino-4,5,6,7-tetrahydro-6-(n-propylamino)benzothiazole. The invention also relates to the methods and intermediates associated with the synthetic process.
专利号:US-8519148-B2 优先权日:2007-03-14 标题 :Synthesis of chirally purified substituted benzothiazole diamines 发明人:RAJE PRASAD; GADIKOTA RAJENDRAKUMAR REDDY; CHEN JIAN-XIE; LAPINA OLGA V; MCCALL JOHN M 权利人:RAJE PRASAD; GADIKOTA RAJENDRAKUMAR REDDY; CHEN JIAN-XIE; LAPINA OLGA V; MCCALL JOHN M; KNOPP NEUROSCIENCES INC 摘要:Methods for preparing chirally purified substituted 4,5,6,7-tetrahydro-benzothiazole diamines such as, for example, (6R)2-amino-4,5,6,7-tetrahydro-6-(propylamino)benzothiazole and purifying a dominant enantiomer of substituted 4,5,6,7-tetrahydro-benzothiazole diamines from entantiomerically enriched mixtures of substituted 4,5,6,7-tetrahydro-benzothiazole diamines are provided herein.
专利号:US-2013079526-A1 优先权日:2010-03-03 标题:Synthesis of Chirally Purified Substituted Benzothiazole Diamines 发明人:GREENFIELD SCOTT JEFFREY; GIBB CAMERON SEATH; GADIKOTA RAJENDRA KUMAR REDDY 权利人:GREENFIELD SCOTT JEFFREY; GIBB CAMERON SEATH; GADIKOTA RAJENDRA KUMAR REDDY; KNOPP NEUROSCIENCES INC 摘要:Methods for preparing chirally purified substituted 4,5,6,7-tetrahydro-benzothiazole diamines such as, for example, (6R)2-amino-4,5,6,7-tetrahydro- 6 -(propylamino)benzothiazole and purifying a dominant enantiomer of substituted 4,5,6,7-tetrahydro-benzothiazole diamines from entantiomerically enriched mixtures of substituted 4,5,6,7-tetrahydro-benzothiazole diamines are provided herein.
专利号:AU-2008224844-B2 优先权日:2007-03-14 标题:Synthesis of chirally purified substituted benzothiazole diamines