Kaneka Corporation

Akio Fujii

Masaru Mitsuda

Kenji Inoue

Kazumi Okuro

Yasuhiro Saka

Masanobu Sugawara

Yasuyoshi Ueda

Tadashi Moroshima

Yoshihide Fuse

Shigeru Kawano

Koichi Kinoshita

Nobuo Nagashima

Toshihiro Takeda

Shohei Yamamoto

Tatsuyoshi Tanaka

Susumu Amano

Hironori Takata

Hiroyuki Ogino

Hirofumi Maeda

Naohiro Imai

Mitsuji Akazawa

Masaya Mizutani

Rie Tanaka

It is an object of the present invention to provide a patch having practical adhesive force and cohesive force as a pharmaceutical product, and also exhibiting a fast-acting anesthetic action. The present invention provides a patch formed from an adhesive layer comprising 5% by weight or more and less than 20% by weight of a mixture of lidocaine and another local anesthetic, wherein the adhesive layer comprises at least a rubber-based pressure-sensitive adhesive and liquid paraffin and a content of a tackifier in the adhesive layer is 10% by weight or less.

Patch

The present application relates to a method for producing an optically active &#x3b1;-amino acid derivative, comprising steps of reacting an &#x3b1;-haloester derivative represented by the general formula (1): of which alcohol part of the ester group is an optically active alcohol derivative,with an amine compound; then deprotecting the obtained compound; further carrying out an ester exchange reaction. According to the present invention method, it is possible to easily produce an optically active &#x3b1;-amino acid ester derivative which is useful as an intermediate for drugs with high selectivity.

Method for producing optically active amino acid derivative

The present invention relates to a method for producing a 2'-hydroxy-protected nucleoside derivative by reacting a ribonucleoside with an acylating or a carbamoylating reagent in the presence of a metal complex consisting of a copper compound and an optically active ligand. By the method according to the present invention, a 2&#x2032;-hydroxy-protected ribonucleoside derivative, which is an important intermediate for producing an oligonucleoside, can be easily produced with good regioselectivity from a nucleoside derivative of which 2&#x2032;,3&#x2032;-hydroxy groups are not protected.

2'-hydroxy-protected ribonucleoside derivative and production method thereof

The present invention has its object to provide a method for producing an optically active hydroxycarboxylic acid derivative which is an intermediate important for production of medicines, agrochemicals, chemical products, and so on. The production method of the present invention comprises: carrying out a hydrogen-transfer reduction of a ketocarboxylic acid or a salt thereof by the reaction of an optically active diamine complex to produce an optically active hydroxycarboxylic acid derivative. According to the present invention, it is possible to safely and efficiently produce an industrially-useful optically active hydroxycarboxylic acid derivative.

Method for producing optically active hydroxycarboxylic acid derivatives or salts thereof

The objective of the present invention is to provide an optically active imidazolidinone derivative widely usable for synthesizing an optically active amino acid, a method of easily producing the derivative, and a method of easily producing an optically active amino acid by using the derivative. The objective can be achieved by producing an optically active amino acid using a novel optically active imidazolidinone derivative represented by a general formula (3) and the like. According to the method of the present invention, an optically active imidazolidinone derivative can be obtained by preferential crystallization from a mixture of isomers of the imidazolidinone derivative. Therefore, an optically active amino acid can be easily and stereoselectively produced without cumbersome procedures required for the conventional methods, such as resolution of diastereomers, synthesis from an optically active amino acid and resolution of isomers by silica gel column chromatography.

Imidazolidinone derivative, method of producing the same and method of producing optically active amino acid

An optically active amino acid derivative is produced by N-protecting an optically active 3-haloalanine derivative followed by cyclization, or cyclizing this derivative followed by N-protection to thereby give an optically active N-protected-aziridine-2-carboxylic acid derivative which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent, or by N-protecting an optically active 3-haloalanine derivative to thereby give N-protected-aziridine-2-carboxylic acid which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent. According to this process, natural and unnatural optically active amino acids can be produced from inexpensive materials by using simple procedures.

Process for producing optically active amino acid derivatives

Process for preparing optically active amino acid derivatives

Process for producing norstatin derivatives

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Takasago, Japan

Akio Fujii