PRODUCTION OF OPTICALLY ACTIVE 2-METHYLPIPERAZINE

    公开(公告)号:JPH04128270A

    公开(公告)日:1992-04-28

    申请号:JP28467690

    申请日:1990-10-22

    Abstract: PURPOSE:To readily obtain the subject compound useful as an intermediate for synthesis of medical drugs such as a quinolone-based antibacterial agent in high yield at a low cost by optically dissolving (RS)-2-methylpiperazine using an optically active N-substituted dicarboxylic acid. CONSTITUTION:An optically active N-substituted dicarboxylic acid represented by the formula ((n) is 1-2; R is acetyl, benzoyl, benzenesulfonyl or p- toluenesulfonyl) is used as an optical resolution agent and brought into contact with (RS)-2-methylpiperazine in a solvent such as methanol. The resultant mixture solution is subsequently cooled and/or concentrated to deposit sparingly soluble diastereomer salts and the residual mother liquid is cooled after concentration or without any treatment to deposit readily soluble diastereomer salts. As the N-substituted dicarboxylic acid as the resolution agent, N-acetylglutamic acid, etc., are exemplified and used in an amount of 0.1-1.5mol based on 1mol (RS)-2-methylpiperizine.

    PRODUCTION OF L-HOMOPHENYLALANINE

    公开(公告)号:JPH03112491A

    公开(公告)日:1991-05-14

    申请号:JP24883789

    申请日:1989-09-25

    Abstract: PURPOSE:To produce L-homophenylalanine useful as a raw material for a precursor of ACE inhibitor, having high optical purity, efficiently and inexpensively by treating benzyllactic acid with a culture mixture or cells of bacterium having specific action. CONSTITUTION:Benzyllactic acid (substrate concentration: about 0.1-5%) is aerobically treated with a culture mixture of a bacterium such as Corynebacterium glutamicum ATCC 13032 belonging to at least one of Corynebacterium, Brevibacterium, Bacillus, Microbacterium, Citrobacter and Arthrobacter or, capable of converting benzyllactic acid into L- homophenylalanine, or cells or treated material thereof at preferably 25-35 deg.C at pH7.5-9.5 and L-homophenylalanine is isolated from the reaction solution and collected.

    NOVEL PLATINUM(II)COMPLEX AND REMEDY FOR MALIGNANT TUMOR

    公开(公告)号:JPH01165594A

    公开(公告)日:1989-06-29

    申请号:JP32649787

    申请日:1987-12-22

    Abstract: NEW MATERIAL:A compound expressed by formula I. USE:A remedy for malignant tumor having low toxicity. PREPARATION:N-(4-Carboxylphenyl)maleimide expressed by formula II is reacted with dihydroxodiaminocyclohexane platinum (II) expressed by formula III, normally under ordinary temperature and ordinary pressure in an aqueous solution to provide the compound expressed by formula I. Furthermore, the compound expressed by formula III which is a starting raw material is produced by heating N-(4-carboxyphenyl)maleimide in an acetic anhydride solvent in the presence of sodium acetate. The compound expressed by formula III is produced by reacting a compound expressed by the formula K2PtCl4 with a compound expressed by formula IV, reacting the resultant compound expressed by formula V with AgNO3 and then treating the resultant compound expressed by formula VI with a OH type anion exchange resin.

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