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    PREPARATION OF NEURAMINIDASE INHIBITOR
    2.
    发明专利
    PREPARATION OF NEURAMINIDASE INHIBITOR 失效

    公开(公告)号：JP2001031631A

    公开(公告)日：2001-02-06

    申请号：JP2000171482

    申请日：2000-06-08

    Applicant: HOFFMANN LA ROCHE

    Inventor： KARPF MARTIN ,  TRUSSARDI RENE

    IPC: B01J31/12 ,  C07B61/00 ,  C07C209/14 ,  C07C209/16 ,  C07C209/52 ,  C07C211/25 ,  C07C211/36 ,  C07C211/40 ,  C07C213/04 ,  C07C213/08 ,  C07C215/20 ,  C07C217/52 ,  C07C231/12 ,  C07C233/03 ,  C07C233/41 ,  C07C233/52 ,  C07C309/66 ,  C07C317/48 ,  C07C317/50

    Abstract: PROBLEM TO BE SOLVED: To obtain a specific diamino compound useful as a viral or bacterial neuraminidase inhibitor without using an azide reagent and azide intermediate through various reactions such as reaction between a specific epoxide and specific amine. SOLUTION: This compound of formula V is obtained by such processes that a compound of formula I (R1, R1', R2, and R2' are each H, an alkyl or the like, but only one of them is H) is reacted with a compound of the formula R5NHR6 (R5 and R6 are each H or an amino substituent, but both of them is not H at the same time) to form a compound of formula II, which is converted to a compound of formula III, which is converted to a compound of formula IV; the free-amino functional group at position 1 of the compound of formula IV is acylated to form the corresponding acylated 1,2-diamino compound and then the amino group at position 2 of the above diamino compound is freed; if necessary, the compound of formula V (R3 and R4 are each H or an amino substituent but both of them are not H at the same time) thus obtained is further converted to the corresponding pharmaceutically acceptable addition salt.

    PRODUCTION OF MIXED ANHYDRIDES
    3.
    发明专利
    PRODUCTION OF MIXED ANHYDRIDES 失效

    公开(公告)号：JPH10175955A

    公开(公告)日：1998-06-30

    申请号：JP33896397

    申请日：1997-12-09

    Applicant: HOFFMANN LA ROCHE

    Inventor： KARPF MARTIN ,  TRUSSARDI RENE

    IPC: C07D215/48 ,  C07C51/56 ,  C07C227/18 ,  C07C227/30 ,  C07C229/02 ,  C07C229/06 ,  C07C271/22 ,  C07D211/44 ,  C07D211/46 ,  C07D217/24 ,  C07D401/12

    Abstract: PROBLEM TO BE SOLVED: To simply prepare the subject mixture useful in activation reaction and coupling reaction without requiring treatment and purification caused by formation of by-product, by adding an adjuvant base to a mixture of an acid and a reactive acid derivative. SOLUTION: A carboxylic acid is mainly used as the acid and an acid halide of the acid is used as the reactive acid derivative. Pivaloyl chloride, isovaleroyl chloride and ethyl chloroformate are especially suitable as the acid halide. A tertiary amine such as triethylamine is used as the adjuvant base. The reaction is carried out in an inert solvent such as a lower carboxylic acid ester at -25 to 25 deg.C to give the objective mixture. For example, the reaction of an anhydride of the formula obtained by reacting a quinoline-2-carboxylic acid with a reactive derivative of the formula R -COOH (R is an alkyl group, etc.) with asparagine gives an intermediate useful for producing a pharmacologically active compound.

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