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    PRODUCTION OF IMIDAZOLE DERIVATIVE
    1.
    发明专利
    PRODUCTION OF IMIDAZOLE DERIVATIVE 失效

    公开(公告)号：JPH08176154A

    公开(公告)日：1996-07-09

    申请号：JP33780994

    申请日：1994-12-26

    Applicant: FUJISAWA PHARMACEUTICAL CO

    Inventor： KAWAKAMI RYOICHI ,  ICHIHARA MASAHARU ,  KODERA TETSUO ,  MORINAGA YASUHIRO ,  NISHIWAKI MASANORI

    IPC: C07D471/04 ,  A61K31/435 ,  A61P43/00

    Abstract: PURPOSE: To safely produce an imidazole derivative having a pharmacological action such as angiotensin II antagonistic action on an industrial scale at a low cost by subjecting a specific compound to a reaction to introduce a lower alkyl group. CONSTITUTION: A compound of formula I (R to R are each a lower alkyl; R is H or an imino-protecting group) is subjected to a lower-alkyl introduction reaction to obtain the objective compound of formula II (R is a lower alkyl), e.g. 5,7-dimethyl-2-hydroxy-3-[4-[1-ethyl-5-methyl-3-(1H-tetrazol-5-yl)-2- pyrrolyl]benzyl]-3H-imidazo[4,5-b]pyridine. The reaction is carried out e.g. in the presence of a lower alkyl iodide (e.g. methyl iodide) and a base such as alkali metal hydroxide (e.g. NaOH) in a solvent such as dioxane.

    NEW PRODUCTION METHOD FOR PEPTIDE COMPOUND
    2.
    发明专利
    NEW PRODUCTION METHOD FOR PEPTIDE COMPOUND 失效

    公开(公告)号：JP2003171395A

    公开(公告)日：2003-06-20

    申请号：JP25974299

    申请日：1999-09-14

    Applicant: FUJISAWA PHARMACEUTICAL CO

    Inventor： ICHIHARA MASAHARU ,  MACHITANI KOJI ,  MORINAGA YASUHIRO ,  KAWAI NOBUTAKA ,  IKE KAZUO

    IPC: C07D401/06 ,  C07K1/02 ,  C07K5/06

    Abstract: PROBLEM TO BE SOLVED: To provide a new production method for a peptide compound (I) in an industrial scale. SOLUTION: This method produces the peptide compound expressed by formula (III) [R 1 , R 2 and R 3 have each the same meaning to the followings] or its salts by reacting a compound expressed by formula (I) or its reactive derivative of an amino group or its salt [R 2 is a lower alkyl group, R 3 is an ar(lower)alkyl group], with a compound expressed by formula (II) or its reactive derivative of the carboxyl group or its salt [R 1 is a lower alkyl group]. COPYRIGHT: (C)2003,JPO

    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.

    PRODUCTION OF PYRROLIDINE COMPOUND OR ITS SALT
    8.
    发明专利
    PRODUCTION OF PYRROLIDINE COMPOUND OR ITS SALT 失效

    公开(公告)号：JPH04346971A

    公开(公告)日：1992-12-02

    申请号：JP21943191

    申请日：1991-05-21

    Applicant: FUJISAWA PHARMACEUTICAL CO

    Inventor： HIRABAYASHI SATOSHI ,  IKE KAZUO ,  ZANKA ATSUHIKO ,  KAWAKAMI TAKESHI ,  ICHIHARA MASAHARU

    IPC: C07D207/14

    Abstract: PURPOSE:To obtain the title compound useful as an intermediate for synthesizing antifungal agents by reaction of dimethyl (S)-N-t-butoxycarbonylaspartate with methyl iodide followed by reduction and then reaction with an amine. CONSTITUTION:Reaction is made in a solvent such as hexane under cooling to heating between (A) a compound of formula I (R a is aminoprotecting group; R and R are each carboxyl-protecting group) and (B) a compound of formula R -X (R is lower alkyl; X is eliminable group) in the presence of a base (e.g. butyllithium) into a compound of formula II, which is then treated with a reducing agent (e.g. hydrogenated sodium boride) into a compound of formula III. Thence, this compound is reacted with a compound of formula H2N-R a (R a is amino-protecting group) in a solvent such as methylene chloride under cooling to heating followed by, when needed, deprotection, thus obtaining the objective compound of formula IV.

    PRODUCTION OF OPTICALLY ACTIVE PIPERIDINEACETIC ACID DERIVATIVE
    9.
    发明专利
    PRODUCTION OF OPTICALLY ACTIVE PIPERIDINEACETIC ACID DERIVATIVE 失效

    公开(公告)号：JPH08333339A

    公开(公告)日：1996-12-17

    申请号：JP14144495

    申请日：1995-06-08

    Applicant: FUJISAWA PHARMACEUTICAL CO

    Inventor： ICHIHARA MASAHARU ,  YAMAZAKI HIROSHI ,  FUKAGAWA MASAYASU ,  KAWAKAMI RYOICHI

    IPC: C07D211/34 ,  C07B57/00

    Abstract: PURPOSE: To obtain a compound useful as an intermediate for producing a compound which is an excellent adenosine antagonist, useful in the field of medicine industry and having extremely high optical purity in good yield. CONSTITUTION: This optically active piperidineacetic acid derivative, e. g. (R)-2-(2-piperidyl)acetic acid benzyl ester.L-tartaric acid salt can be produced by leading a racemic modification of a piperidineacetic acid derivative such as 2-(2-piperidyl)acetic acid expressed by the formula (R is a protected carboxy group such as benzyloxycarbonyl group) to a diastereomer using an optically active acid such as L-tartaric acid, D-mandelic acid or D-10-camphorsulfonic acid, carrying out fractional crystallization of the diastereomer and as necessary further, decomposing the separated crystal to the resolving reagent and the original compound.

    PRODUCTION OF 5-AMINOPYRAZOLE DERIVATIVE
    10.
    发明专利
    PRODUCTION OF 5-AMINOPYRAZOLE DERIVATIVE 失效

    公开(公告)号：JPH07206826A

    公开(公告)日：1995-08-08

    申请号：JP29632294

    申请日：1994-11-30

    Applicant: FUJISAWA PHARMACEUTICAL CO

    Inventor： HIRABAYASHI SATOSHI ,  ICHIHARA MASAHARU ,  FUJII YOSUKE ,  KODERA TETSUO

    IPC: C07D231/38

    Abstract: PURPOSE:To exclusively obtain a 5-aminopyrazole derivative in high selectivity and yield by using a 2-substituted taminomethylene-2-cyanoacetic acid compound as a starting substance and reacting with a hydrazine derivative. CONSTITUTION:A 5-aminopyrazole derivative of formula I can be produced by reacting a 2-substituted aminomethylene-2-cyanoacetic acid compound of formula II (R is a substituted amino; R is a protected carboxy) or its salt with a compound of formula III (R is a lower hydroxyalkyl) or its salt. The compound of formula II used as a starting substance can be produced by reacting a compound of formula IV or its salt with a compound of formula V and a compound of formula VI (R is a lower alkyl). The objective compound having excellent safety can be produced since the compound of formula II is free from skin irritation. Since the compound of formula II is producible from an inexpensive compound, this process is advantageous also from the viewpoint of cost. The compound of formula I is useful as a raw material for a cephalosporin compound known as an excellent antibiotic substance.

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