174483-06-8Relevant articles and documents
A fexofenadine hydrochloride process for synthesizing
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, (2017/02/17)
The invention discloses a synthetic process of fexofenadine hydrochloride. The synthetic process of fexofenadine hydrochloride comprises the following steps of: with alpha, alpha-dimethyl phenylacetic acid as a raw material, carrying out an esterification reaction on alpha, alpha-dimethyl phenylacetic acid and absolute ethyl alcohol under the catalysis of a silica gel loaded phosphotungstic acid (PW12/SiO2) solid acid catalyst to obtain alpha, alpha-dimethyl ethyl phenylacetate; carrying out Friedel-Grafts reaction on alpha, alpha-dimethyl ethyl phenylacetate and 4-chlorobutyryl chloride to obtain alpha, alpha-dimethyl-4-(4-chloro-1-oxo butyl) ethyl phenylacetate; reducing by virtue of sodium borohydride in 95% ethyl alcohol to obtain alpha, alpha-dimethyl-4-(4-chloro-1-hydroxyl butyl) ethyl phenylacetate; and carrying out N-alkylation reaction on alpha, alpha-dimethyl-4-(4-chloro-1-hydroxyl butyl) ethyl phenylacetate and alpha, alpha-dimethyl-4-piperidine methyl alcohol in DMF (dimethyl formamide) for 24 hours at the temperature of 80 DEG C to obtain alpha, alpha-dimethyl-4-[1-hydroxyl-4-[4-(hydroxyl diphenylmethyl)-1-piperidyl]-butyl] ethyl phenylacetate, and then carrying out alkali hydrolysis and salification by virtue of hydrochloric acid, so that fexofenadine hydrochloride is obtained. The synthetic process of fexofenadine hydrochloride is high in yield and low in cost, produces less pollution and is applicable to industrial mass production.
Combination of dehydroepiandrosterone or dehydroepiandrosterone-sulfate with an antihistamine for treatment of asthma or chronic obstructive pulmonary disease
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, (2008/06/13)
A pharmaceutical or veterinary composition, comprises a first active agent selected from a dehydroepiandrosterone and/or dehydroepiandrosterone-sulfate, or a salt thereof, and a second active agent comprising an antihistamine for the treatment of asthma, chronic obstructive pulmonary disease, or any other respiratory disease. The composition is provided in various formulations and in the form of a kit. The products of this patent are applied to the prophylaxis and treatment of asthma, chronic obstructive pulmonary disease, or any other respiratory disease.
Process and diastereomeric salts useful for the optical resolution of racemic a-[4- (1,1-dimethylethy) phenyl) -4- (hydroxydipenylmethyl) -1-piperidinebutanol and derivative compounds
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, (2008/06/13)
A process and diastereomeric salts useful for the optical resolution of racemic alpha-[4-(1,1-dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebutanol, 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-alpha,alpha-dimethylbenzeneacetic acid and lower alkyl 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-alpha,alpha-dimethylbenzeneacetates. The process comprises placing into solution a chiral resolving agent, either (+)/(-)-di-paratoluoyltartaric acid or (-)/(+)-mandelic acid, in an amount equimolar to a compound corresponding to the desired enantiomer of the above compound, precipitating the resulting diastereomeric salt between the chiral resolving agent and the target enantiomer and separating the enantiomer.