- Phenylethanolamine β receptor agonist synthetic method
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The invention discloses a phenylethanolamine β receptor agonist synthetic method, comprises the following steps: S1: the 4 - amino acetophenone dissolved in an organic solvent, with the electrophilic reagent occurs on the benzene ring substituted halogenated reaction, generating [...] intermediate; [...] intermediates in organic solvent or in water, under the catalysis of the metal catalyst with the cyanide reagent undergo nucleophilic substitution reaction, generating phenyl ketone intermediate; S2: phenyl ketone intermediates in organic solvent, with the copper bromide generating carbonyl α bromo reaction to produce α - bromoacetophenone intermediates; S3: α - bromoacetophenone intermediates in organic solvent with tert-butyl amine or isopropylamine reaction intermediates acetophenone amines; S4: acetophenone amine intermediates in organic solvent, with the reduction hydrogenation reagent react to generate the phenylethanolamine β receptor agonists; synthetic method of this invention a simple and highly efficient and cheap and easy to obtain, atom utilization is high, the synthetic product chemical purity is greater than 99%, to meet the detection requirements of the food safety.
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Paragraph 0065; 0075-0080
(2019/07/04)
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- Raising of pigs
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The fat content of sows' milk is increased, thereby increasing the energy supplied to the sow's piglets, by administering one of a small group of phenethanolamines.
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- Repartitioning Agents: 5--anthranilonitrile and Related Phenethanolamines; Agents for Promoting Growth, Increasing Muscle Accretion and Reducing Fat Deposition in Meat-producing Animals
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A series of phenethanolamines related to clenbuterol was prepared and examined in mice for growth-promoting and fat-reducing activities.Several analogs were equipotent to clenbuterol.In chickens, 5-anthranilonitrile appeared to be more potent than clenbuterol with recpect to "repartitioning" activity, that is, the ability to redirect food energy from fat formation to muscle accretion.Based on this potency and low residue levels in edible tissues, this compound is in advanced stages of evaluation for commercial use in meat animals.
- Asato, Goro,Baker, Pamela K.,Bass, Roy T.,Bentley, T. James,Chari, Sarangan,et al.
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p. 2883 - 2888
(2007/10/02)
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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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- Phenylethanolamine derivatives and acid addition salts thereof for enhancing the growth rate of meat-producing animals and improving the efficiency of feed utilization thereby
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There is provided a method for enhancing the growth rate of meat-producing animals and/or improving the efficiency of feed utilization thereby, which involves, orally or parenterally, administering to said animals a growth-enhancing amount of a phenylethane compound or the acid addition salt thereof.
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- Phenylethanolamine derivatives and acid addition salts thereof for the depression of fat deposition in warm blooded animals
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There is provided a method for increasing lean meat deposition and/or improving lean meat to fat ratio in poultry, domestic pets, sheep, swine, rabbits, goats and cattle by administering, orally or parenterally, to said animals an effective amount of a phenylethane derivative or acid salt thereof.
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- BRONCHOSPASMOLYTIC 1-(P-AMINO-PHENYL)-2-AMINO-ETHANOLS-(1) AND SALTS
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Racemic and optically active compounds of the formula wherein R1 is hydrogen, fluorine, chlorine, bromine, iodine or cyano, R2 is fluorine, trifluoromethyl, nitro or cyano, and R3 is alkyl of 3 to 5 carbon atoms, hydroxy(alkyl of 3 to 5 carbon atoms), cycloalkyl of 3 to 5 carbon atoms, 1-(3,4-methylenedioxy-phenyl)-2-propyl or 1-(p-hydroxy-phenyl)-2-propyl, and non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as analgesics, uterospasmolytics, bronchospasmolytics and antispastics for the skeletal musculature, and especially as beta 2-receptor mimetics and beta 1-receptor blockers
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