Nippon Shinyaku Company, Ltd.

Toshio Tomita

Masahiro Kise

Hiromu Murai

Masahiko Kitano

Koji Kitaguchi

Akira Sano

Tatsuo Suminokura

Hiroshi Nishida

Hiroshi Enomoto

Yoshiaki Aoyagi

Shoichi Chokai

Kiyoshi Kimura

Iwao Morita

Masami Tsuda

Kenichi Nakamura

Takashi Okubo

Koyishi Kimura

Massahiro Kise

Shoicho Chokai

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.

Process for producing pyrimidine derivative and intermediate thereof

Pyroglutamide derivatives have been found to be useful as nootropic agents for administration to humans and animals.

Pyroglutamide derivatives

A compound of formula (I): ##STR1## wherein R.sup.1 is alkenyl or alkyl or both of the depicted R.sup.1 groups together represent trimethylene and form a six-membered ring together with the depicted oxygen and phosphorus atoms, R.sup.2 is nitro, trifluoromethyl or halogen, R.sup.3 is alkyl, and R.sup.4 is dimethoxymethyl, formyl, hydroxymethyl or nitrile.

Certain antihypertensive 1,4-dihydro-6-methyl-5-phosphonic

1-phenoxy-3-(4-phenylpiperazino)-2-propanol derivatives of the formula (I): ##STR1## and pharmaceutically acceptable salts thereof wherein R.sup.1 is hydrogen, halo or lower alkyl; R.sup.2 is pyrrolidino, piperidino, morpholino or perhydroazepino unsubstituted or substituted by carbonyl at the alpha-position; R.sup.3 is hydrogen, lower alkyl or lower alkoxycarbonyl; and R.sup.4 is hydrogen, lower alkyl unsubstituted or alpha-substituted by lower alkoxy, lower alkoxy, halo or lower alkanoyl are useful for their alpha and beta-adrenergic blocking action and their hypotensive activity in humans and animals.

1-phenoxy-3-(4-phenylpiperidino)-2-propand having both alpha- and

Steryl-6-0-palmitoyl-.beta.-D-glucosides are anti-inflammatory agents. The compounds, of which .beta.-sitosteryl-6-0-palmitoyl-.beta.-D-glucoside is a representative embodiment, are prepared through the reaction of a steryl-6-0-sulfonyl-.beta.-D-glucoside with an alkali metal salt of palmitic acid.

Steryl-.beta.-D-glucoside esters and method of preparation

Steryl-6-O-palnitoyl and -2,3,4,6-O-tetrapalmitoyl-.beta.-D-glucosides are anti-inflammatory agents. The compounds, of which .beta.-sitosteryl-2,3,4,6-O-tetrapalmitoyl-.beta.-D-glucoside is a representative embodiment, are prepared through the reaction of a steryl-.beta.-D-glucoside with a lower alkyl ester of palmitic acid in the presence of a basic catalyst.

Steryl-.beta.-D-glucoside ester pharmaceutical compositions and method

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Kusatsu, Japan

Toshio Tomita