CAS: 67287-36-9; 2-(2-Chloro-3,4-Dimethoxyphenyl)Ethanamine

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2-氯-1-(氯甲基)-3,4-二甲氧基苯置于硼烷体系中,用 四氢呋喃,二甲基亚砜 作为反应溶剂,化学反应 2.75H,反应生成 2-氯-3,4-二甲氧基苯乙胺
参考文献:多巴胺激动剂1-芳基-2,3,4,5-四氢-1H-3-苯并ze庚因-7,8-二醇的合成及其肾脏血管舒张活性:非诺多old的卤素和甲基类似物.
标题:多巴胺激动剂1-芳基-2,3,4,5-四氢-1H-3-苯并ze庚因-7,8-二醇的合成及其肾脏血管舒张活性:非诺多old的卤素和甲基类似物.
摘要:发现某些6-卤代-1-苯基-2,3,4,5-四氢-1H-3-苯并ze庚因是有效的d-1多巴胺激动剂.1-(4-羟苯基)类似物不具有中枢神经系统活性,因为它们的高极性抑制了其进入大脑.但是,这些化合物是有效的肾血管扩张药.非氯多巴,6-氯类似物,是该系列中特别重要的成员,其合成,药理和临床特性已得到广泛研究.6-甲基和6-碘同系物是有效的肾血管扩张剂,但通过刺激大鼠尾状腺苷酸环化酶测定,非有效的部分d-1激动剂.可能的合理化建议这些活动具有不同的受体储备.9位取代的苯并庚因多巴胺激动剂不活跃或效力低下,
DOI:10.1021/jm00161A029

专利信息

专利号:US-4172890-A
优先权日:1977-04-01
标 题 :2,3,4,5-Tetrahydro-1H-3-benzazepine-7,8-diones
发明人：HOLDEN KENNETH G
权利人:SMITHKLINE CORP
摘要:Novel benzazepine derivatives having central and peripheral dopaminergic activity useful in treating Parkinson's and cardiovascular diseases. The compounds have additional use as intermediates for the synthesis of other benzazepines with similar useful properties. The 1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-dione derivatives are particularly useful.

专利号:US-4108989-A
优先权日:1977-04-01
标 题 :2,3,4,5-tetrahydro-1h-3-benzazepine-7,8-diones
发明人：HOLDEN KENNETH GEORGE
权利人:SMITHKLINE CORP
摘要:Novel benzazepine derivatives having central and peripheral dopaminergic activity useful in treating Parkinson's and cardiovascular diseases. The compounds have additional use as intermediates for the synthesis of other benzazepines with similar useful properties. The 1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-dione derivatives are particularly useful.

专利号:US-4285938-A
优先权日:1979-10-11
标 题:7,8-Dihydroxy-1-(sulfamylphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine derivatives
发明人：PFEIFFER FRANCIS R
权利人:SMITHKLINE CORP
摘要:New 7,8-dihydroxy-1-(sulfamylphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepines having pharmaceutical activity together with new intermediates and methods of synthesis for preparing them. The lead compound is 6-chloro-7,8-dihydroxy-1-(p-sulfamylphenyl)-2,3,4,5-tetrahydro-1H-3-be nzazepine which has very potent renal dopaminergic activity.