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    METHOD FOR CONTINUOUSLY PRODUCING SUBSTITUTED OXAZOLE
    4.
    发明专利
    METHOD FOR CONTINUOUSLY PRODUCING SUBSTITUTED OXAZOLE 审中-公开

    公开(公告)号：JP2003201283A

    公开(公告)日：2003-07-18

    申请号：JP2002227742

    申请日：2002-08-05

    Applicant: BASF AG

    Inventor： RUST HARALD ,  BURKART KIRSTEN ,  FAUST TILLMANN ,  HENKELMANN JOCHEM ,  KINDLER ALOIS ,  KNOLL CHRISTIAN ,  MOHRY ANDRE

    IPC: C07D213/67 ,  C07D263/42

    Abstract: PROBLEM TO BE SOLVED: To provide a method for continuously producing a 5-alkoxy-substituted oxazole and a method for producing a pyridoxine derivative by using the same. SOLUTION: This method for obtaining a pyridoxine derivative is provided by converting an α-isocyanoalkanoic acid ester expressed by the formula II in the presence of continuously supplied base at ≥80°C temperature to a 5- alkoxy-substituted oxazole I, taking it out from a reactor at the same time with the reaction, performing a reaction of the compound I with a compound VI to make a compound VII, and acid-treating it to obtain a pyridoxine derivative IX (in formulae, R 1 is an alkyl, R 2 is H or an alkyl, R 3 , R 4 are each independently a protection group of hydroxy group). COPYRIGHT: (C)2003,JPO

    METHOD FOR PRODUCING SUBSTITUTED OXAZOLE
    5.
    发明专利
    METHOD FOR PRODUCING SUBSTITUTED OXAZOLE 审中-公开

    公开(公告)号：JP2003176272A

    公开(公告)日：2003-06-24

    申请号：JP2002227292

    申请日：2002-08-05

    Applicant: BASF AG

    Inventor： RUST HARALD ,  BURKART KIRSTEN ,  FAUST TILLMANN ,  HENKELMANN JOCHEM ,  KINDLER ALOIS ,  KNOLL CHRISTIAN ,  BECKER MICHAEL

    IPC: C07D233/70 ,  C07D213/67 ,  C07D263/42

    Abstract: PROBLEM TO BE SOLVED: To provide a method for producing a 5-alkoxy-substituted oxazole and a method for producing a pyridoxine derivative. SOLUTION: The 5-alkoxy-substituted oxazole is obtained by converting an α-isocyano alkylic acid ester in the presence of a base at >80°C and separating the 5-alkoxy-substituted oxazole from the reaction mixture simultaneously with the converting reaction, and the pyridoxine derivative is obtained by converting an amino acid into an amino acid ester, converting the obtained into a formamido acid ester, converting the obtained into an α-isocyanoalkyl acid ester, converting the obtained into a 5-alkoxy-substituted oxazole in the presence of a base at >80°C and separating the 5-alkoxy-substituted oxazole from the reaction mixture simultaneously with the converting reaction, reacting the obtained 5-alkoxy-substituted oxazole with a protective diol to obtain an Diels-Alder adduct and treating the obtained with an acid and removing the protective group to convert into the pyridoxine derivative. COPYRIGHT: (C)2003,JPO

    PRODUCTION OF ORTHOESTER
    6.
    发明专利
    PRODUCTION OF ORTHOESTER 失效

    公开(公告)号：JP2000159716A

    公开(公告)日：2000-06-13

    申请号：JP35637199

    申请日：1999-11-10

    Applicant: BASF AG

    Inventor： BURKART KIRSTEN ,  GUTH JOSEF ,  LETZELTER THOMAS ,  SCHWEINZER JUERGEN ,  STERZEL HANS-JOSEF

    IPC: C07C41/60 ,  C07C43/32

    Abstract: PROBLEM TO BE SOLVED: To provide a method for producing an orthoester in a high yield, by reacting a trihaloalkane with an alkali metal alkoxide in the presence of a corresponding alcohol using a slurry of the alkali metal alkoxide. SOLUTION: This method for producing an orthoester comprises reacting (A) a 1,1,1-trihaloalkane (for example, 1,1,1-trihalomethane) with (B) an alkali metal alkoxide, for example, sodium methoxide, in the presence of a corresponding alcohol using a slurry (a suspension of the solid alkali metal alkoxide in the alcohol) by use of, for example, a blade drier, a kneader and a discotherm reactor. The slurry is preferably used in a state that a weight ratio of the solid component to the dissolved alkali metal alkoxide is at least 0.4. The reaction is preferably carried out using the component A in an amount of at most 1.1 mol per 3 mol of the component B.

    8.
    发明专利
    未知

    公开(公告)号：DE50211588D1

    公开(公告)日：2008-03-13

    申请号：DE50211588

    申请日：2002-07-26

    Applicant: BASF AG

    Inventor： RUST HARALD ,  BURKART KIRSTEN ,  FAUST TILLMANN DR ,  HENKELMANN JOCHEM DR ,  KINDLER ALOIS DR ,  KNOLL CHRISTIAN DR ,  MOHRY ANDRE DR

    IPC: C07D263/42

    Abstract: Continuous production of 5-alkoxy oxazoles (I) comprises heating an alkyl alpha -isocyanoalkanoate ester (II) at a temperature above 80 degrees C in the presence of an auxiliary agent and withdrawing the product from the reactor. Continuous production of 5-alkoxy oxazoles of formula (I) comprises heating an alkyl alpha -isocyanoalkanoate ester of formula (II) at a temperature above 80 degrees C in the presence of an auxiliary agent and withdrawing the product from the reactor. R1 = optionally substituted 1-6C alkyl; R2 = H or optionally substituted 1-6C alkyl. An Independent claim is also included for a process for producing pyridoxine derivatives of formula (IX), comprising: (1) converting an amino acid of formula (III) to an ester of formula (IV); (2) converting (IV) to a formamido ester of formula (IV); (3) converting (IV) to (II); (4) converting (II) to (I) as above; (5) reacting (I) with a protected diol of formula (VI) to form a Diels-Alder adduct of formula (VII); and (6) converting (VII) to (IX) by acid treatment and deprotection. R3, R4 = protecting groups or together form a protecting group.

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