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2 - (heterocycloalkoxy) - 1 - (subst. - phenyl) - ethanol derivatives as active ingredients for improving cerebral potentiality for function

机译:2-(杂环烷氧基)-1-(取代基-苯基)-乙醇衍生物作为有效成分,可改善大脑功能的潜力

摘要

1-Phenyl-2-substd. oxy-ethanol derivs. of formula R1CH(OR2)CHR3-O-(CR4R5)n-R6 (I) and their salts are new; n is 0-6; R1 is phenyl (opt. substd. by (i) halogen, (ii) NQ1Q2, (iii) alkyl, acryl, aralkyl, alkoxy, aralkoxy, aryloxy, carbamoyloxy, alkylthio, alkenyl, alkenyloxy, aralkylthio, aralkylsulphonyl, arylsulphonyl, alkylsulphonylamino, arylsulphonylamino or Het, (all opt. substd.), or (iv) protected amino, opt. protected hydroxy, NO2, oxo or lower alkylenedioxy); R2 is H, alkyl or hydroxy-protecting gp.; R3-R5 are H or alkyl; R6 is ammonio, NQ1Q2 or Het; Het is N-bonded heterocyclic gp. e.g., pyrrolyl, pyrrolidinyl, piperidyl, piperazinyl, imidazolyl, pyrazolyl, pyridyl, tetrahydropyridyl, pyrimidinyl, morpholinyl, thiomorpholinyl, quinolyl, quinolizinyl, tetrahydroquinolyl, etc.; Q1, Q2 are H, opt. protected OH, alkyl (opt. substd. by opt. protected OH or opt. protected COOH), cycloalkyl, aryl, lower acyl, aralkyl, Het1, Het1-O-CO- (opt. substd. by oxo), adamantyl, alkylsulphonyl or arylsulphonyl; Het1 is N-contg. heterocycle as for Het; or e.g. furyl, thienyl, benzothienyl, pyranyl, isobenzofuraryl, imidazo(2,3-a)pyridyl, benzo(b)piperazinyl, chromenyl, isothiazolyl, isoxazolyl, oxadiazolyl, pyridazinyl, isoindolyl or isoquinolyl, etc.; all alkyl and alkenyl moieties are lower, i.e., up to 6C; with provisos.
机译:1-苯基-2-取代氧-乙醇衍生物。式R1CH(OR2)CHR3-O-(CR4R5)n-R6(I)的式子及其盐是新的; n为0-6; R1是苯基(由(i)卤素,(ii)NQ1Q2,(iii)烷基,丙烯酸,芳烷基,烷氧基,芳烷氧基,芳氧基,氨基甲酰氧基,烷硫基,烯基,烯基氧基,芳烷硫基,芳烷基磺酰基,芳基磺酰基,烷基磺酰基氨基,芳基磺酰基氨基或Het(均全选),或(iv)受保护的氨基,经选择保护的羟基,NO2,氧代或低级亚烷基二氧基); R 2为H,烷基或羟基保护基。 R3-R5为H或烷基; R6是铵,NQ1Q2或Het; Het是N键合的杂环gp。例如吡咯基,吡咯烷基,哌啶基,哌嗪基,咪唑基,吡唑基,吡啶基,四氢吡啶基,嘧啶基,吗啉基,硫代吗啉基,喹啉基,喹啉嗪基,四氢喹啉基等; Q1,Q2是H,opt。受保护的OH,烷基(由受保护的OH取代或由受保护的COOH取代),环烷基,芳基,低级酰基,芳烷基,Het1,Het1-O-CO-(由氧代取代),金刚烷基,烷基磺酰基或芳基磺酰基; Het1是N-contg。像Het一样的杂环;或例如呋喃基,噻吩基,苯并噻吩基,吡喃基,异苯并呋喃基,咪唑并(2,3-a)吡啶基,苯并(b)哌嗪基,色烯基,异噻唑基,异恶唑基,恶二唑基,哒嗪基,异吲哚基或异喹啉基等;所有的烷基和烯基部分均较低,即至多6℃;附带条件。

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