CAS: 59311-67-0; 2-(3-Thienyl)Ethylamine

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📜3-甲基噻吩置于n-溴代丁二酰亚胺(Nbs),Lithium Aluminium Tetrahydride,苄基三乙基氯化铵,过氧化苯甲酰体系中,用 四氢呋喃,水 作为反应溶剂,化学反应生成 3-氨乙基噻吩
参考文献:D 1-样受体,可区分硫杂a嗪区域异构体
标题:D 1-样受体,可区分硫杂a嗪区域异构体
摘要:由于受体螺旋内的高度同一性,设计具有d 1 / D 5亚型选择性的配体是一项挑战.基于先导化合物1-3,合成了噻吩-苯并ze庚因区域异构体4和5,并使用放射性配体结合亲和力技术对它们对五种多巴胺受体亚型的亲和力进行了生物学评估.内的d 1样家族,化合物4显示出对d 20倍的选择性5亚型超过d 1亚型(ķ我= 3Nm时,D 1:60纳米),而它的区域异构体,化合物5用颠倒噻吩位置,更喜欢d 1在d亚型5亚型(ķ我= 4Nm的,D 5:15纳米).苯并噻吩并-苯并ze庚因类似物6被证明是对d 1-和d 2-样家族成员具有相同亲和力的几个数量级(a D 2和1.9的k I = 1.5 Nm)具有高亲和力的a嗪衍生物之一.d 5为nm).彻底分析构成目标多巴胺受体亚型结合口袋的氨基酸残基,发现在d 5 通过阴离子氨基酸稳定的丝氨酸s 6.62和苏氨酸t 7.33残基或水网络的受体可能有助于合成化合物的选择性模式.
DOI:10.1039/c5Md00258C

专利信息

专利号:US-4876362-A
优先权日:1986-12-23
标题:Process for the preparation of thienylethylamines
发明人：RADISSON JOEL; BRAYE EMILE
权利人:SANOFI SA
摘要:The invention has as its subject a process for the preparation of thienylethylamines of the formula n n R--NR--R' n n where R represents the group ##STR1## and R' represents hydrogen or a group identical to R, by catalytic hydrogenation of a compound of the formula ##STR2## synthesis intermediates.

专利号:US-6369222-B1
优先权日:2000-07-18
标题 :mGluR antagonists and a method for their synthesis
发明人：BINGGELI ALFRED; MAERKI HANS-PETER; MUTEL VINCENT; WOSTL WOLFGANG; WILHELM MAURICE
权利人:HOFFMANN LA ROCHE
摘要:The invention relates to nitro- and cyano-1,2,4,5-tetrahydro-heterocycloazepinyl pyrimidine derivatives as well as their pharmaceutically acceptable salts. The invention further relates to medicaments containing such compounds and a process for the preparation of such compounds. The compounds of the invention are group I mGluR antagonists and are therefore useful for the control or prevention of acute and/or chronic neurological disorders.