- 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 0081-0088
(2019/07/04)
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- Compositions and methods for inducing adipose tissue cell death
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Pharmaceutical compositions, methods for increasing the rate of apoptosis in adipose tissue cells, and methods of reducing adipose tissue mass in a host, are described. One exemplary pharmaceutical composition, among others, includes at least one catecholamine in combination with a pharmaceutically acceptable carrier. The catecholamine is present in a dosage level effective to increase the rate of apoptosis in adipose tissue cells in a host.
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- Separation of enantiomers of cimaterol, (-)-cimaterol and the use thereof in animal feeds
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The invention relates to the separation of enantiomers, of cimaterol, (-)-cimaterol, the addition salts thereof and processes for preparing them and their use in pharmaceutical compositions and animal feeds.
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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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- Method for increasing weight gains and reducing deposition of fat in animals
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The invention is a novel method comprising administering growth hormones parenterally and substituted phenylethane derivatives orally or parenterally to meat producing animals to obtain increased weight gains and anti-lipogenic activity in the animals.
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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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- 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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- 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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