Shionogi Company Limited

Astrazeneca Ab

Shionogi Seiyaku Kabushiki Kaisha

Haruo Koike

Makoto Kobayashi

Masahiko Nagai

Kentaro Hirai

Teruyuki Ishiba

Mikio Kabaki

Masamichi Watanabe

Nigel Phillip Taylor

Loius J Diorazio

Shoji Shinomoto

Yoshinori Hamada

Yutaka Nishino

Makoto Kakinuma

Nigel Philip Taylor

Isamu Yamada

Louis Joseph Diorazio

Katsuo Oda

Koji Matsuda

Yasufumi Ueda

A process for a preparation of Compound (V), a pharmaceutically acceptable salt or a solvate thereof, said process comprising the steps represented by the following formula: wherein Rand Rare each independently C&#x2013;Calkyl.

Process for producing triterpene derivative

A method for producing a compound represented by the general formula (I-A) or the general formula (I-B), comprising the following step: wherein Ris an optionally substituted lower alkyl, and the like; Ris a lower alkyl or an optionally substituted aralkyl, and the like; Ris a lower alkyl, characterized in that a compound represented by the general formula (II-A) or the general formula (II-B) is treated with thionyl chloride.

Processes for the preparation of oxo-oxazoline or alloamino acid derivatives

A method for producing a compound represented by the general formula (I-A) or the general formula (I-B), comprising the following step:wherein Ris an optionally substituted lower alkyl, and the like; Ris a lower alkyl or an optionally substituted aralkyl, and the like; Ris a lower alkyl, characterized in that a compound represented by the general formula (II-A) or the general formula (II-B) is treated with thionyl chloride.

The invention concerns a process for the manufacture of tert-butyl (E)-(6-[2-4-(4-flourophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl]vinyl)-(4R,6S)-2,2-dimethyl[1,3]-dioxan-4-yl)acetate, the novel starting material used in said process and the use of the process in the manufacture of a pharmaceutical.

Process for the production of tert-butyl (E)-(6-[2-[4-(4-flurophenyl)-6-isopropyl-2-[methyl(methylsufonyl)amino]pyrimidin-5-yl]vinyl]4R,6S)-2,2-dimethyl[1,3]dioxan-4-yl)acetate

The invention concerns a process for the manufacture of tert-butyl (E)-(6-&lsqb;2-4-(4-fluorophenyl)-6-isopropyl-2-&lsqb;methyl(methylsulfonyl)amino&rsqb;pyrimidin-5-yl&rsqb;vinyl)-(4R, 6S)-2,2-dimethyl(1,3-dioxan-4-yl) acetate, the novel starting material used in said process and the use of the process in the manufacture of a pharmaceutical.

Process for the production of tert-butyl (E)-(6-&lsqb;2-&lsqb;4-(4-fluorophenyl)-6-isopropyl-2-&lsqb;methyl(methylsulfonyl)amino&rsqb;pyrimidin-5-yl&rsqb;vinyl&rsqb;(4R,6S)-2, 2-dimethyl&lsqb;1, 3&rsqb;dioxan-4-yl)acetate

The compounds of the present invention inhibit the HMG-CoA reductase, and subsequently suppress the biosynthesis of cholesterol. And they are useful in the treatment of hypercholesterolemia, hyperlipoproteinemia, and atherosclerosis.

Pyrimidine derivatives

Process for producing carbamoylmethylurea derivatives

The compounds of the present invention inhibit HMG-CoA reductase, and subsequently suppress the synthesis of cholesterol. And they are useful in the treatment of hypercholesterolemia, hyperlipoproteinemia, and atherosclerosis. The compounds have the formula ##STR1## wherein R.sup.1, R.sup.2, and R.sup.3 each is independently hydrogen, optionally substituted lower alkyl, or optionally substituted aryl; R.sup.4 is lower alkyl, aralkyl, aryl, or heteroaryl, each of which is optionally substituted; X is vinylene or ethylene; Y is ##STR2## where R.sup.5 is hydrogen, lower alkyl, aryl, aralkyl, or a cation capable of forming a non-toxic pharmaceutically acceptable salt.

Pyrrole derivatives

An improved process for preparing a vinyl imidazole derivative (I) and a new method of production of a monoimidazole derivative (II) are provided: ##STR1## wherein R.sup.1 is halogen; and R.sup.2, X, and Y are each is hydrogen or halogen. The vinyl imidazole derivatives (I) are useful as antimycotic agents for humans and animals or agricultural fungicides, and the monoimidazole derivatives (II) can be utilized as intermediates for preparing them.

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Hyogo, Japan

Haruo Koike