- Novel arylethanolamines for promoting livestock production
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The growth of livestock is promoted by the novel arylethanolamines of the formula STR1 in which R1 represents cyano, R2 represents amino, alkylamino or acylamino, R3 represents hydrogen, halogen, alkyl, halogenoalkyl, alkoxy, halogenoalkoxy, hydroxymethyl, nitro or methylsulphonylmethyl, R4 represents hydrogen, alkyl or acyl, R5 represents hydrogen or alkyl, R6 represents alkyl, n represents 1, 2 or 3, R7 represents the radicals --COR9, --O-alkylene-COR9, -alkylene-R10 or --O-alkylene-R10, R8 represents hydrogen, alkyl or halogen, R9 represents hydroxyl, alkoxy or the radical --NR11 R12, R10 represents hydroxyl, alkoxy or the radical NR11 R12, R11 represents hydrogen or alkyl, and R12 represents hydrogen or alkyl, and the physiologically acceptable salts thereof.
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- Synthesis of further amino-halogen-substituted phenyl-aminoethanols
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Starting from clenbuterol as a lead structure, new 4-amino-phenyl-aminoethanol analogues have been synthesized by different approaches. In these compounds one or both of the chlorine atoms of clenbuterol are replaced by other residues. This has led to compounds with high intrinsic β2-mimetic and/or β1-blocking activities. 1-(4-Amino-3-chloro-5-trifluoromethyl-phenyl)-2-tert.-butylamino-ethanol hydrochloride (mabuterol) has been selected for clinical development. A detailed description is also given of the syntheses of new intermediate acetophenone derivatives as well as of the resolution of mabuterol into its enantiomers.
- Kruger,Keck,Noll,Pieper
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p. 1612 - 1624
(2007/10/02)
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