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    PRODUCTION OF DIALKOXYACETIC ACID ESTER COMPOUND
    4.
    发明专利
    PRODUCTION OF DIALKOXYACETIC ACID ESTER COMPOUND 失效

    公开(公告)号：JPS6248648A

    公开(公告)日：1987-03-03

    申请号：JP19067585

    申请日：1985-08-28

    Applicant: FUJISAWA PHARMACEUTICAL CO

    Inventor： YAZAWA HISATOYO ,  HASHIMOTO NORIO ,  KAKARA KOUJI

    IPC: C07C69/708 ,  C07C67/27

    Abstract: PURPOSE:To obtain the titled compound useful as a synthetic intermediate for 1,4-dihydropyridine compound which is useful as a medicine, under mild condition in high yield in single step reaction, by using glyoxylic acid as a starting compound and reacting the acid with an ortho ester. CONSTITUTION:Glyoxylic acid of formula or its salt is used as a starting compound and is made to react with an ortho ester of formula II (R is lower alkyl or lower alkoxy-lower alkyl) in a non-aqueous solvent such as methanol under moderate heating or heating at about the boiling point of the solvent to obtain the objective compound of formula III. The amount of the compound of formula II is preferably 3-5mol, especially about 4mol per 1mol of the compound of formula I. the above reaction is carried out preferably in the presence of a catalyst such as hydrogen chloride, sulfuric acid, acetic acid, methanesulfonic acid, etc. The amount of the acid is between catalytic amount and 2mol, preferably about 0.1mol per 1mol of glyoxylic acid used as a raw material.

    NEW PRODUCTION ROUTE FOR N-MONOACYLPIPERAZINE
    6.
    发明专利
    NEW PRODUCTION ROUTE FOR N-MONOACYLPIPERAZINE 失效

    公开(公告)号：JP2000128874A

    公开(公告)日：2000-05-09

    申请号：JP30054398

    申请日：1998-10-22

    Applicant: FUJISAWA PHARMACEUTICAL CO

    Inventor： ICHIHARA MASAHARU ,  HASHIMOTO NORIO ,  BABA YUKIHISA ,  KODERA TETSUO ,  KANDA ATSUSHI

    IPC: C07D295/16

    Abstract: PROBLEM TO BE SOLVED: To obtain the subject novel N-monoacylpiperazine in high yield by effecting the N-acylation reaction in the presence of two NH groups without the N-protection of one NH group in the (homo)piperazine by allowing specific two compounds to react with each other. SOLUTION: (A) A compound of formula I (n is 2, 3) and (B) a compound of formula II [R1 is a (substituted) lower alkyl, a (substituted) aryl, a (substituted) heterocyclic ring; R2 is a (substituted) aryl] are allowed to react with each other in a solvent with heat under pressure to give a compound of formula III. Etyl acetate, toluene, acetonitrile, dioxane, tetrahydrofuran and the like can be used as a solvent. This production process can be utilized as an industrial production process for N-monoacyl(homo)piperazine and a part of production process for manufacturing the medicines having this chemical skeleton.

    NEW PRODUCTION
    7.
    发明专利
    NEW PRODUCTION 失效

    公开(公告)号：JPH10175914A

    公开(公告)日：1998-06-30

    申请号：JP33945396

    申请日：1996-12-19

    Applicant: FUJISAWA PHARMACEUTICAL CO

    Inventor： ICHIHARA MASAHARU ,  HASHIMOTO NORIO ,  KODERA TETSUO ,  BABA YUKIHISA

    IPC: C07D249/18 ,  C07C51/08 ,  C07C63/38 ,  C07D295/14 ,  C07D521/00

    Abstract: PROBLEM TO BE SOLVED: To enable the obtaining of a high-purity carboxylic acid compound useful as a synthetic raw material, etc., for a lipopeptide antifungal agent in high yield at a low cost without forming hardly separable by-products by hydrolyzing a specific higher alkoxy-containing nitrile compound. SOLUTION: The hydrolytic reaction of (A) a compound represented by formula I [R is a 3-6C alkoxy or a higher alkoxy, preferably the 3-6C alkoxy; A and A are each an aromatic ring or a heterocyclic ring, preferably benzene; X is a single bond, an aromatic ring, a heterocyclic ring or a (cyclo)-lower alkane, preferably piperazine] or its salt is carried out to afford a compound represented by formula II or its salt. The reaction is conducted in the presence of a base or an acid in, e.g. water, a hydrophilic organic solvent or a mixed solvent thereof at 70-150 deg.C temperature.

    NEW PRODUCTION OF PYRAZOLOPYRIDINE
    8.
    发明专利
    NEW PRODUCTION OF PYRAZOLOPYRIDINE 失效

    公开(公告)号：JPH069631A

    公开(公告)日：1994-01-18

    申请号：JP12092893

    申请日：1993-04-23

    Applicant: FUJISAWA PHARMACEUTICAL CO

    Inventor： NAKAMURA HITOSHI ,  KAWAKAMI RYOICHI ,  YAMAZAKI HIROSHI ,  HASHIMOTO NORIO ,  TAKI ISAO

    IPC: C07D471/04

    Abstract: PURPOSE:To obtain a new method for producing a pyrazolopyridine compound useful as an intermediate for producing pyrazolopyridine derivatives useful as medicines. CONSTITUTION:A compound of formula III (R is lower alkyl; R is H or proper substituent group), e.g. 1-phenyl-1-butyn-3-one is made to react with a compound of formula II (R is H or proper substituent group; X is anion), e.g. N- aminopyridine iodide in a polar solvent such as N,N-dimethylformamide or dimethyl sulfoxide at ambient temperature to 50 deg.C to provide the objective compound of formula I, e.g. 3-acetyl-2-phenylpyrazolo[1,5-a]pyridine.

    NEW PRODUCTION PROCESS
    9.
    发明公开
    NEW PRODUCTION PROCESS 失效
    NEHES HUNTELLUNGSVERFAHREN

    公开(公告)号：EP0994101A4

    公开(公告)日：2002-05-02

    申请号：EP98924609

    申请日：1998-06-15

    Applicant: FUJISAWA PHARMACEUTICAL CO

    Inventor： ICHIHARA MASAHARU ,  HASHIMOTO NORIO ,  KANDA ATSUSHI ,  KAGARA KOOJI

    IPC: C07C227/06 ,  C07C229/34 ,  C07C229/38 ,  C07D261/08

    CPC classification number: C07C227/06 ,  C07C229/38 ,  C07C229/34

    Abstract: A new process for producing compounds of general formula (I), wherein R1 is carboxyl or protected carboxyl; R2 is lower alkoxyl or higher alkoxyl; and A?1 and A2¿ are each an aromatic divalent group, a heterocyclic divalent group or a cyclo(lower)alkylene group or salts of them, characterized by producing compounds of general formula (II), wherein R?1, R2, A1 and A2¿ are eachas defined above or salts thereof from compounds of general formula (III), wherein R?1, R2, A1 and A2¿ are each as defined above or salts thereof and producing compounds of general formula (I) from those of formula (II) or salts thereof.

    Abstract translation: 本发明涉及一种制备下式（I）化合物的新方法。 因此，制备式（I）的化合物的方法：其中R 1是羧基或被保护的羧基; R 2是低级烷氧基或更高级烷氧基; A 1是二价芳环，二价杂环基或二价环（低级）烷烃; 并且A 2是二价芳族环，二价杂环基或二价环（低级）烷烃或其盐，其包括使式（III）化合物：其中R 1，R 2， 2>，A 1和A 2各自如上所定义，或其盐与酸性铵盐反应，得到式（II）的化合物：其中R 1，R 2 >，A 1和A 2各自如上所定义，或其盐，进一步与羟胺盐反应。

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