Fujisawa Pharmaceutical Company, Ltd.

Daicel Chemical Industries, Ltd.

Tokuyama Corporation

Nagasaki University

Osamu Onomura

Masahiro Nishikawa

Hiroshi Kayakiri

Noritsugu Yamasaki

Hitoshi Sawada

Takafumi Imoto

Takahiro Hiramura

Teruo Kyoto Oku

Yoshito Abe

Hitoshi Hamashima

Yoichiro Ueda

Tsuyoshi Mizutani

Fumiaki Iwasaki

Yoshihiro Matsumura

Ichiro Takase

Toshiharu Yanagi

Yoshiyuki Murai

Kenji Tanaka

Kazuya Kodama

Akira Katayama

Yutaro Tsuda

Masami Kuriyama

Provided is a process for producing an optically active compound represented by Formula (3): (wherein Ris an alkyl group, an alkynyl group, an alkenyl group, an aliphatic heterocyclic group, a cycloalkyl group, an aryl group, an aralkyl group, or an aromatic heterocyclic group, and any hydrogen atom of Rmay be replaced with a substituent; Ris a hydrogen atom or a group which is not reactive in the reaction below; and * represents a chiral center) or a salt thereof by subjecting a compound represented by Formula (1): (wherein Rand Rhave the same meanings as defined in Formula (3)) to a ring closure reaction in the presence of a chiral ligand having 1 or more coordination sites, a Lewis acid represented by Formula (2):MZ&#x2003;&#x2003;(2)(wherein M is a metal ion, Z is a counter anion of M, and m and n are integers of 1 to 4), and a sulfonyl halide having an optionally substituted alkyl or phenyl group.

Method for producing optically active compound or salt thereof

The present invention discloses a process for producing an aliphatic dicarboxylic acid compound, which comprises oxidizing, with a nitrite or a nitrate in the presence of trifluoroacetic acid, an alicyclic secondary alcohol compound or an alicyclic ketone compound, in each of which at least one methylene group is bonded to the carbon atom having hydroxyl group bonded thereto or the carbon atom as a member of carbonyl group, wherein the reaction is conducted in the presence of water of 5 mass % or less relative to 100 mass % of the total of the trifluoroacetic acid and the water.

Process for producing aliphatic dicarboxylic acid compound

A sulfonamide compound of the formula (I):R&#x2014;SONHCO&#x2014;A&#x2014;X&#x2014;R&#x2003;&#x2003;(I)wherein Ris alky, alkenyl, alkynyl and the like; A is an optionally substitutedheteropolycyclic group except benzimidazolyl, indolyl, 4,7-dihydrobenzimidazolyland 2,3-dihydrobenzoxazinyl; X is alkylene, oxa, oxa(lower)alkylene and the like; and Ris optionally substituted aryl, substituted biphenylyl and the like, a salt thereof and a pharmaceutical composition comprising the same. The sulfonamide compound is effective for the diseases treatable based on their blood sugar level-depressing activity, cGMP-PDE (especially PDE-V)-inhibiting activity, smooth muscle relaxing activity, bronchodilating activity, vasodilating activity, smooth muscle cell suppressing activity, and antiallergic activity.

Sulfonamide compounds and pharmaceutical use thereof

Benzimidazole derivatives

A method of preparing a reduced product by efficiently reducing an unsaturated organic compound by using, as a reducing agent, a trichlorosilane which is industrially cheaply available and is easy to handle, and a reducing agent therefor. A reduced product of an unsaturated organic compound is obtained by mixing the unsaturated organic compound and a trichlorosilane together to reduce the unsaturated organic compound in the presence of a compound that forms a silicon complex having five coordinations upon acting on the trichlorosilane such as an N-formylated product of a secondary amine having not less than 3 carbon atoms. The invention further provides a reducing agent comprising a particular silicon complex.

Process for preparing reductants of unsaturated organic compounds by the use of trichlorosilane and reducing agents

Sulfonamide compounds and medicinal use thereof

Novel aromatic ring derivatives represented by formula (I) or their pharmaceutical acceptable salts are provided.

Aromatic ring derivatives

The present invention provides useful intermediates for the synthesis of 2,5-diamino-1,6-diphenyl-3-hydroxyhexane derivatives which serve as intermediates in the synthesis of medicines such as retrovirus protease inhibitors including human immunodeficiency virus (HIV) protease inhibitors, and a method for preparing these intermediates using the former intermediates. More particularly, the invention provides methods for preparing a 2-isoxazoline derivative represented by formula �1! and a 2,5-diamino-1,6-diphenyl-3-hydroxyhexane derivative obtainable by reducing the 2-isoxazoline derivative and represented by formula �6!: ##STR1## (wherein Ph is phenyl; and each of R.sup.1 and R.sup.2 independently represents hydrogen, acyl, alkyloxycarbonyl, arylalkyloxycarbonyl, aryloxycarbonyl, alkylaminocarbonyl, arylalkylaminocarbonyl, arylaminocarbonyl, alkyl, arylalkyl, aryl, alkylsulfonyl, arylalkylsulfonyl, or arylsulfonyl, or R.sup.1 and R.sup.2 are linked to each other to represent divalent acyl).

2-isoxazoline derivative and process for producing the same, and process

Growing community of inventors

Nagasaki, Japan

Osamu Onomura