| 摘要 |
1286161 Pyridoxine mono-esters SOC D'ETUDES DE PRODUITS CHIMIQUES 19 April 1971 [21 Jan 1970 3 Sept 1970] 2899/70 and 42153/70 Heading C2V Salts of pyridoxine mono-ester have the formula where A and A<SP>1</SP> are alkylene radicals or divalent amino-substituted aliphatic hydrocarbon radicals, R<SP>1</SP> and R<SP>2</SP> are alkyl radicals or together with the nitrogen atom form a heterocyclic ring, AC is a pharmaceutically acceptable acid, and n is 1, 2 or 3. The compounds are prepared by blocking the two alcohol functions in the 3- and 4- positions of pyridoxine, reacting the compound thus obtained with an acyl chloride of formula to obtain an intermediate of formula removing the blocking group R, e.g. by hydrolysis, and reacting the resulting compound with a pharmaceutically acceptable acid to obtain the addition salt. In examples pyridoxine is reacted with acetone to block the two alcohol functions; the acyl chlorides used are the acyl chloride of dimethylamino ethanol mono-succinate, the acyl chloride of dimethylamino ethanol monoglutarate and the acyl chloride of N-methyl N<SP>1</SP>- ethanol piperazine mono-succinate; the blocked alcohol groups are liberated by hydrolysis with formic acid; and the salts are obtained by reaction with maleic acid and with N-acetyl aspartic acid. The salts may be mixedwith pharma ceutically acceptable diluents and carriers. |
