- Fexofenadine hydrochloride of synthetic method
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The invention discloses a fexofenadine hydrochloride synthesizing method. The fexofenadine hydrochloride synthesizing method comprises the steps of taking 2-(4-bromophenyl)-2-methylpropionate (2) as a raw material, enabling the 2-(4-bromophenyl)-2-methylpropionate (2) to react with nafoxidine to protect a carboxyl, and then reacting with [gamma]-butyrolactone to generate a compound 6, enabling the compound 6 to react with paratoluensulfonyl chloride, condensing a product and a [alpha], [alpha]-diphenyl-4-(Hydroxymethyl)-piperidine, and finally obtaining a target compound 1 through reduction and deprotection. The raw materials selected by the way are cheap to obtain; furthermore, the synthesizing method is mild in reaction condition, convenient to operate and smaller in environmental pollution, therefore the fexofenadine hydrochloride synthesizing method is an industrial way with a better application prospect.
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- Intermediates useful for the preparation of antihistaminic piperidine derivatives
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The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula whereinW represents —C(=O)— or —CH(OH)—;R1 represents hydrogen or hydroxy;R2 represents hydrogen;R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2;n is an integer of from 1 to 5;m is an integer 0 or 1;R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof,with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy, m is an integer 0.
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Page column 103
(2010/01/30)
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