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6 - Lower - alkyl - 7,8 - dihydroxy - 1 - phenyl - 2,3,4,5 - tetrahydrofuran - 1h - 3 - benz azepines as well as their salts with acids and their use as a dopaminergic active ingredients
6 - Lower - alkyl - 7,8 - dihydroxy - 1 - phenyl - 2,3,4,5 - tetrahydrofuran - 1h - 3 - benz azepines as well as their salts with acids and their use as a dopaminergic active ingredients
6-Lower alkyl-7, 8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines of formula: CHEM in which: R is a lower alkyl of 1-6 carbons; R1 is hydrogen, benzyl, phenethyl, lower alkanoyl of 1-5 carbons, lower alkyl of 1-5 carbons, lower alkyenyl of 3-5 carbons, furyl methyl, thienylmethyl or phenacyl; R2 and R3 are each hydrogen, lower alkyl of 1-5 carbons, lower alkanoyl of 2-5 carbons, benzyl or, when taken together, methylene; and R4 is hydrogen or one or two substituents from the group comprising trifluoromethyl, halo, methyl, methoxy, acetoxy, hydroxy or methylthio; or pharmaceutically acceptable, acid addition salts thereof show dopaminergic activity. Intermediates and chemical methods for preparing them are described. An important species is 6-methyl-7,8-dihydroxy-1(p-hydroxyphenyl) -2,3,4,5- tetrahydro -1H-3-benzazepine, as the base or one of its salts, which has antihypertensive activity.
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机译:式:的6-低级烷基-7,8-二羟基-1-苯基-2,3,4,5-四氢-1H-3-苯并ze庚因,其中:R是1-6个碳的低级烷基; R1是氢,苄基,苯乙基,1-5个碳的低级烷酰基,1-5个碳的低级烷基,3-5个碳的低级炔基,呋喃基甲基,噻吩基甲基或苯甲酰基; R 2和R 3各自为氢,1-5个碳的低级烷基,2-5个碳的低级烷酰基,苄基或当合在一起时为亚甲基; R4是氢或选自三氟甲基,卤素,甲基,甲氧基,乙酰氧基,羟基或甲硫基的一个或两个取代基;或其药学上可接受的酸加成盐显示出多巴胺能活性。描述了制备它们的中间体和化学方法。重要的物质是6-甲基-7,8-二羟基-1(对羟基苯基)-2,3,4,5-四氢-1H-3-苯并ze庚因,为碱或其盐之一,具有降压活性。
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