Process for producing pyrimidine derivative and intermediate...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C544S242000

Reexamination Certificate

active

07091206

ABSTRACT:
The present invention relates to a method for producing a pyrimidine derivate useful as a neurocyte neurocyte necrosis inhibitor and an intermediate thereof. Disclosed is a method for producing an acid salt of 4-(4-fluorophenyl)-2-methyl-6-(5-piperidinopentyloxy) pyrimidine. The method comprises reacting 4-chloro-6-(4-fluorophenyl)-2-methylpyrimidine with 5-piperidino-1-pentanol, hydrating the thus obtained 4-(4-fluorophenyl)-2-mehtyl-6-(5-piperidinopentylox) pyrimidine and then converting the resultant the hydrate into an acid salt. The hydrate as a describe above; and a method for producing the hydrate is part of this invention. According to 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 a industrial scale.

REFERENCES:
patent: 5945426 (1999-08-01), Chokai et al.
patent: 6191149 (2001-02-01), Chokai et al.
“Na+ and high-voltage activated Ca2+ channel blocking actions of NS-7, a novel neuroprotective agent, in NG108-15 cells.” Suma et al. European Journal of Pharmacology 336 (1997) pp. 283-290.

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