Shionogi Company Limited

Shionogi Seiyaku Kabushiki Kaisha

Kyozo Kawata

Mitsuaki Ohtani

Yoshio Hamashima

Masayuki Narisada

Fumihiko Watanabe

Yusuke Suzuki

Toyohiko Takeda

Teruo Sakamoto

Kyoji Minami

Masanori Tujikawa

Bunji Kageyama

Takayasu Sonoyama

Masaaki Uenaka

Masahiko Nagai

Takeshi Endoh

Mikio Kabaki

Makoto Kakinuma

Masanori Nakae

Shoichi Hirai

Toshiaki Masui

Takemasa Hida

Takayuki Kasai

Disclosed is a method for oxidizing an alcohol in an amide solvent using a mixed reagent containing hydrogen peroxide and a tungsten catalyst.

Oxidation of alcohol with use of hydrogen peroxide and tungsten catalyst

A process for producing amidine derivatives represented by the following reaction scheme, characterized in that the reactions of steps 1 and 3 are conducted in acetonitrile and the reaction of step 2 is conducted in acetone.

Process for preparation of amidine derivatives

Industrial and commercial processes for the preparation of 2-acyl-5-benzylfuran derivatives, 1,2,4-triazole-3-carboxylic acid ester derivatives or propenone derivatives having an anti-HIV activity; and useful crystals of the derivatives. A deblocking: (III-2), (IV-10), (VI-1), wherein R , R and R are each independently hydrogen or the like; A is CR or N; R is hydrogen or the like; Q is a protecting group; and L is a leaving group.

Processes for the preparation of substituted propenone derivatives

Method for producing optically active norborneol by ester hydrolysis

A process suitable for industrially preparing 2,3-trans-1,4-bridged cyclohexane sulfonamide derivatives, especially useful as an intermediate for the synthesis of a trans bicyclo[2,2,1] heptane carboxylic acid derivative, a clinically important thromboxane A.sub.2 antagonist, comprising: allowing to react corresponding a cis/trans mixture of sulfonamide derivatives with an anionoid or water-soluble carbonyl reagent at pH 3-7 so that the trans isomer may form a water-soluble adduct with the anionoid or carbonyl reagent, separating the resulting adduct dissolved in an aqueous layer, and recovering the trans isomer by treating the adduct with a base or an acid. Also provided is an alkali metal hydrogen sulfite adduct of 2,3-trans 1,4-bridged cyclohexane sulfonamide derivative.

Intermediates for preparation of 2,3-trans-1,4-bridged cyclohexane

A process suitable for industrially preparing 2,3-trans-1,4-bridged cyclohexane sulfonamide derivatives, especially useful as an intermediate for the synthesis of a trans bicyclo[2,2,1] heptane carboxylic acid derivative, a clinically important thromboxane A.sub.2 antagonist, comprising: allowing to react corresponding a cis/trans mixture of sulfonamide derivatives with an anionoid or water-soluble carbonyl reagent at pH3-7 so that the trans isomer may form a water-soluble adduct with the anionoid or carbonyl reagent, separating the resulting adduct dissolved in an aqueous layer, and recovering the trans isomer by treating the adduct with a base or an acid. Also provided is an alkali metal hydrogen sulfite adduct of 2,3-trans 1,4-bridged cyclohexane sulfonamide derivative.

Preparation of 2,3-trans-1,4-bridged cyclohexane sulfonamide derivatives

An antibacterial, 7.beta.-[(Z)-2-(2-aminothiazol-4-yl)-4-carboxybut-2-enoylamino]-3-cephem-4 -carboxylic acid is stable in a (di or tri)-hydrate crystal form. A pharmacologically effective amount of this hydrate is filled in a gelatin hard capsule and sealed by a band of gelatin to make a stable composition for clinical use after storage for a long time.

Gelatin hard capsule containing crystalline hydrate of oral cephalosporin

A process for preparing a compound of Formula (I): ##STR1## wherein R is phenyl or phenyl substituted with hydroxy, lower alkoxy, halogen or lower alkyl; Y is unsubstituted or substituted methylene, ethylene, vinylene or oxygen; m is 0 or 1; n is 0, 1 or 2; and q is 1, 2, 3 or 4; with the limitation that when m is 0, n is not 0, and when m is 1, n is not 2, which process comprises:

Process for preparing 1,4-bridged cyclohexane carboxylic acid derivatives

Method for preparing crystalline hydrate of oral celphalosporin and its

An antibacterial, 7.beta.-[(Z)-2-(2-aminothiazol-4-yl)-4-carboxybut-2-enoylamino]-3-cephem-4 -carboxylic acid is stable in a (di or tri)-hydrate crystal form. A pharmacologically effective amount of this hydrate is filled in a gelatin hard capsule sealed by a band of gelatin to make a stable composition for clinical use after storage for a long time.

Crystalline hydrate of oral cephalosporin and its composition

A phenylisoxazole of the formula: ##SPC1## Wherein, Y represents a hydrogen atom, a halogen atom, an alkali metal atom or a tertiary amino group and Z represents a sulfur atom or a sulfoxide group. They are prepared by subjecting 3-alkoxycarbonyl-5-phenylisoxazole to a treatment with at least one agent selected from the group consisting where required and as necessary of dimethyl sulfoxide, a neutralizing agent, an agent capable of releasing a halogen ion and a secondary amine at a temperature ranging from about -5.degree.C to about 70.degree.C for a time period from several minutes up to about 4 hours. The phenylisoxazoles are useful as intermediates for preparing a 3-(2-tertiary amino-1-hydroxyethyl)-5-phenylisoxazole, any of which is known as useful medicaments having a remarkable analgesic, antispasmodic, antiphretic, antiallergic, antiinflammatory, antitussive activity or the like, each reflecting the species of the substituent tertiary amino groups and generally having a very low toxicity.

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Osaka, Japan

Kyozo Kawata