Process for producing pyrimidine derivative and intermediate thereof
AssigneeNippon Shinyaku Co., Ltd.
InventorToshio Tomita
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AssigneeNippon Shinyaku Co., Ltd.
InventorToshio Tomita
Estimating the term…
The present invention relates to a method for producing a pyrimidine derivative useful as a neurocyte necrosis inhibitor and an intermediate thereof. More particularly speaking, a method for producing an acid salt of 4-(4-fluorophenyl)-2-methyl-6-(5-piperidinopentyloxy)pyrimidine comprising reacting 4-chloro-6-(4-fluorophenyl)-2-methylpyrimidine with 5-piperidino-1-pentanol, hydrating the thus obtained 4-(4-fluorophenyl)-2-methyl-6-(5-piperidinopentyloxy)pyrimidine and then converting the resultant hydrate into an acid salt; the hydrate as described above; and a method for producing the hydrate. According to the method of the present invention, a highly pure acid salt of 4-(4-fluorophenyl)-2-methyl-6-(5-piperidinopentyloxy)pyrimidine can be readily and efficiently produced without using a column chromatography. Thus, this method is suitable for the production thereof on an industrial scale.
A method for producing an acid salt of 4-(4-fluorophenyl)-2-methyl-6-(5-piperidinopentyloxy)pyrimidine comprising forming a hydrate of 4-(4-fluorophenyl)-2-methyl-6-(5-piperidinopentyloxy)pyrimidine and then converting into an acid salt.
A hydrate of 4-(4-fluorophenyl)-2-methyl-6-(5-piperidinopentyloxy)pyrimidine.
A method for producing a hydrate of 4-(4-fluorophenyl)-2-methyl-6-(5-piperidinopentyloxy)pyrimidine comprising dissolving 4-(4-fluorophenyl)-2-methyl-6-(5-piperidinopentyloxy)pyrimidine in an acidic aqueous solution and adjusting the solution at pH 7 or higher with a basic aqueous solution.
A method for producing a hydrate of 4-(4-fluorophenyl)-2-methyl-6-(5-piperidinopentyloxy)pyrimidine comprising dissolving 4-(4-fluorophenyl)-2-methyl-6-(5-piperidinopentyloxy)pyrimidine in an organic solvent and distilling the solvent off in the presence of water followed by cooling.
A method for producing a hydrate of 4-(4-fluorophenyl)-2-methyl-6-(5-piperidinopentyloxy)pyrimidine comprising stirring 4-(4-fluorophenyl)-2-methyl-6-(5-piperidinopentyloxy)pyrimidine together with water or an aqueous organic solvent.
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