DITERPENE DERIVATIVE, ITS PRODUCTION AND ANTITUMOR AGENT CONTAINING THE SAME AS ACTIVE INGREDIENT

    公开(公告)号:JPH08245505A

    公开(公告)日:1996-09-24

    申请号:JP22896595

    申请日:1995-09-06

    Abstract: PURPOSE: To obtain a new compound useful as physiologically active substances including technical products of medicines and agrochemicals, their intermediates and antitumor agents. CONSTITUTION: This compound of formula I [R is H or a 1-20C acyloxy; R and R are each H or pivalyl and R and R are each H when R is H, on the other hand, R and R are each H, a 1-20C acyl, a (substituted)benzoyl, a (substituted)benzyl, trityl, etc., when A is the 1-20C acyloxy], e.g. 1,3- oxyingenol 20-trityl ether. The compound of formula I is obtained by reacting a compound of formula II [R is H or a 1-20C acyloxy; R is pivalyl when R is H, on the other hand, R is a 1-20C acyl, a (substituted)benzoyl, a (substituted)benzyl, trityl, etc., when R is a 1-20C acyloxy] with a halide of the formula R X [R is a 1-20C acyl, a (substituted)benzoyl, a (substituted) benzyl, trityl, etc.; X is a halogen].

    106.
    发明专利
    失效

    公开(公告)号:JPH04290847A

    公开(公告)日:1992-10-15

    申请号:JP5525191

    申请日:1991-03-20

    Applicant: DAICEL CHEM

    Inventor: FUJIWA TAKAAKI

    Abstract: PURPOSE:To produce the subject compound having low volatility, odor, viscosity and toxicity in high yield by adding dicyclopentadiene to an easily available acrylate using a catalyst such as heteropoly acid. CONSTITUTION:The objective compound of formula II (e.g. the compound of the formula wherein R is CH3, R is H and n is 1) can be produced by reacting (A) a compound of formula I (R and R are H or CH3; n is integer of 1-20) (e.g. 1mol adduct of epsilon-caprolactone to 2-hydroxyethyl methacrylate) with (B) dicyclopentadiene in the presence of a catalyst consisting of a heteropoly acid or its acidic salt, especially heteropoly acid of tungsten or its acidic salt (particularly 12-tungstophosphoric acid, 12-tungstosilicic acid, 12-tungstoboric acid or their acidic salts). The compound of formula II producible by the above simplified process at a low cost is useful also as coating material, molding material, etc., and reactive diluent for coating material, etc.

    PRODUCTION OF DIALDEHYDE DERIVATIVE
    107.
    发明专利

    公开(公告)号:JPH03236343A

    公开(公告)日:1991-10-22

    申请号:JP3119290

    申请日:1990-02-09

    Abstract: PURPOSE:To obtain the subject compound on an industrial scale at a low cost by epoxidizing an olefin derivative with hydrogen peroxide in the presence of sodium tungstate, phosphoric acid and a phase-transfer catalyst in a binary system containing a non-polar solvent and oxidizing the product with periodic acid. CONSTITUTION:The objective compound of formula III useful as an intermediate for a prostaglandin-like compound can be extremely easily produced in high purity and yield using inexpensive and highly safe hydrogen peroxide and periodic acid by reacting a compound of formula I [one of A and A is H and the other is (CH2)nX or A and A together form a protected CO; n is 1 or 2; X is acetoxy, COOR or OCH2COOR; R is 1-4C straight-chain or branched alkyl] with hydrogen peroxide in the presence of sodium tungstate, phosphoric acid and a phase-transfer catalyst in a binary system containing a non-polar solvent and reacting the resultant compound of formula II with meta-periodic acid in a binary system containing a non-polar solvent.

    PRODUCTION OF MONOESTER DERIVATIVE OF OXALIC ACID

    公开(公告)号:JPH03223231A

    公开(公告)日:1991-10-02

    申请号:JP1980290

    申请日:1990-01-29

    Applicant: DAISO CO LTD

    Abstract: PURPOSE:To obtain the subject compound useful as an intermediate of penem- based antibiotic substance or anti-allergic compound from an inexpensive and to a readily available raw material for a short time in a high yield and high purify by hydrolyzing diesters of oxalic acid using hydrogencarbonate salt of an alkali metal. CONSTITUTION:Diesters of oxalic acid expressed by formula II (R is 1-6C linear or branched alkyl, cycloalkyl, alkenyl, cycloalkenyl, benzyl, methoxybenzyl or nitrobenzyl) are hydrolyzed by using hydrogencarbonate salt expressed by formula III (M is alkali metal) to afford the objective compound expressed by formula I. By said method, the objective compound is obtained in a high yield and high purity for a relatively short time by using a raw material readily available in a low cost without generating by-product such as acetic acid inducing problems in operation and the quality control and suppressing by production of a compound expressed by formula IV generated by further hydrolysis of the objective compound.

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