1.
    发明专利
    未知

    公开(公告)号:AT307820T

    公开(公告)日:2005-11-15

    申请号:AT02738658

    申请日:2002-06-12

    Abstract: Preparation of a 2'-O-acetyl-4''-O-formyl-11-oxo-12-alkoxy-8,9-anhydroerythromycin A 6,9-hemiketal compound (III) comprises reacting a 2'-O-acetyl-4''-O-formyl-11-oxo-8,9-anhydroerythromycin A 6,9-hemiketal compound (I) with an alkylating agent in a mixed solvent comprising 0.18-1.05 equivalents water to (I) and an organic solvent. Preparation of a 2'-O-acetyl-4''-O-formyl-11-oxo-12-alkoxy-8,9-anhydroerythromycin A 6,9-hemiketal compound of formula (III) comprises reacting a 2'-O-acetyl-4''-O-formyl-11-oxo-8,9-anhydroerythromycin A 6,9-hemiketal compound of formula (I) with an alkylating agent in a mixed solvent comprising 0.18-1.05 equivalents water to (I) and an organic solvent. [Image] R 1, R 2lower alkyl.

    2.
    发明专利
    未知

    公开(公告)号:DE60205912D1

    公开(公告)日:2005-10-06

    申请号:DE60205912

    申请日:2002-06-12

    Abstract: Preparation of a 2'-O-acetyl-4''-O-formyl-8,9-anhydroerythromycin A 6,9-hemiketal compound (IV) comprises formylating a 2'-O-acetyl-8,9-anhydroerythromycin A compound (II) to give a 2'-O-acetyl-4''-O-formyl-erythromycin A compound (III); reacting (III) with an acid to give the corresponding hemiketal compound; and adding aqueous base to precipitate (IV) in free form as crystals. Preparation of a 2'-O-acetyl-4''-O-formyl-8,9-anhydroerythromycin A 6,9-hemiketal compound of formula (IV) comprises: (i) formylating a 2'-O-acetyl-8,9-anhydroerythromycin A compound of formula (II) to give a 2'-O-acetyl-4''-O-formyl-erythromycin A compound of formula (III); (ii) reacting (III) with an acid to give the corresponding hemiketal compound; and (iii) adding aqueous base to precipitate (IV) in free form as crystals. [Image] [Image] R1, R2lower alkyl.

    3.
    发明专利
    未知

    公开(公告)号:DE60206921T2

    公开(公告)日:2006-07-20

    申请号:DE60206921

    申请日:2002-06-12

    Abstract: Preparation of a 2'-O-acetyl-4''-O-formyl-11-oxo-12-alkoxy-8,9-anhydroerythromycin A 6,9-hemiketal compound (III) comprises reacting a 2'-O-acetyl-4''-O-formyl-11-oxo-8,9-anhydroerythromycin A 6,9-hemiketal compound (I) with an alkylating agent in a mixed solvent comprising 0.18-1.05 equivalents water to (I) and an organic solvent. Preparation of a 2'-O-acetyl-4''-O-formyl-11-oxo-12-alkoxy-8,9-anhydroerythromycin A 6,9-hemiketal compound of formula (III) comprises reacting a 2'-O-acetyl-4''-O-formyl-11-oxo-8,9-anhydroerythromycin A 6,9-hemiketal compound of formula (I) with an alkylating agent in a mixed solvent comprising 0.18-1.05 equivalents water to (I) and an organic solvent. [Image] R 1, R 2lower alkyl.

    4.
    发明专利
    未知

    公开(公告)号:AT303395T

    公开(公告)日:2005-09-15

    申请号:AT02736057

    申请日:2002-06-12

    Abstract: Preparation of a 2'-O-acetyl-4''-O-formyl-8,9-anhydroerythromycin A 6,9-hemiketal compound (IV) comprises formylating a 2'-O-acetyl-8,9-anhydroerythromycin A compound (II) to give a 2'-O-acetyl-4''-O-formyl-erythromycin A compound (III); reacting (III) with an acid to give the corresponding hemiketal compound; and adding aqueous base to precipitate (IV) in free form as crystals. Preparation of a 2'-O-acetyl-4''-O-formyl-8,9-anhydroerythromycin A 6,9-hemiketal compound of formula (IV) comprises: (i) formylating a 2'-O-acetyl-8,9-anhydroerythromycin A compound of formula (II) to give a 2'-O-acetyl-4''-O-formyl-erythromycin A compound of formula (III); (ii) reacting (III) with an acid to give the corresponding hemiketal compound; and (iii) adding aqueous base to precipitate (IV) in free form as crystals. [Image] [Image] R1, R2lower alkyl.

    5.
    发明专利
    未知

    公开(公告)号:DE69716962T2

    公开(公告)日:2003-07-03

    申请号:DE69716962

    申请日:1997-08-19

    Applicant: UBE INDUSTRIES

    Abstract: The present invention is to provide a trifluoro-substituted benzoic acid, an ester thereof, particularly 2,3,4-trifluoro-5-iodobenzoic acid, 2,3,4-trifluoro-5-trifluoromethylbenzoic acid, esters thereof, which are useful as a starting material for synthesizing a quinolonecarboxylic acid compound useful as a medicine, an anti-bacterial agent or an antiviral agent, and processes for preparing these compounds and 2,4,5-trifluoro-3-iodobenzoic acid, 2,4,5-trifluoro-3-trifluoromethylbenzoic acid and esters thereof.

    7.
    发明专利
    未知

    公开(公告)号:DE60102120D1

    公开(公告)日:2004-04-01

    申请号:DE60102120

    申请日:2001-11-15

    Applicant: UBE INDUSTRIES

    Abstract: The present invention provides a novel 7a-alkoxy-4H-pyrano-Ä3,2-dÜ-oxazol-2(3H)-one represented by the formula (I): wherein R and R each represent a hydrogen atom, an alkyl group, an alkenyl group, an aryl group or an aralkyl group; R represents an alkyl group, a cycloalkyl group, an alkenyl group, an aryl group or an aralkyl group, provided that a 2-alkenyl group is excluded from the alkenyl group of R ; and R represents an alkyl group, an aryl group, an alkoxycarbonyl group or a cyano group, and a process for producing the same which comprises reacting 5-alkoxy-2(3H)-oxazolone with an alpha , beta -unsaturated ketone in the presence of a Lewis acid in a solvent.

    8.
    发明专利
    未知

    公开(公告)号:DE69526443T2

    公开(公告)日:2002-12-12

    申请号:DE69526443

    申请日:1995-10-04

    Applicant: UBE INDUSTRIES

    Abstract: The present invention relates to a 2-silyloxy-4,5,6,7-tetrahydrothienoÄ3,2-cÜpyridine represented by the formula (I): wherein R , R and R each independently represent an alkyl group having 1 to 10 carbon atoms or an aryl group, and a salt thereof and a process for preparing the same, and a 5-alkyl-2-silyloxy-4,5,6,7-tetrahydrothienoÄ3,2-cÜ-pyridine represented by the formula (IV): wherein R , R and R represent the same meanings as described above; R represents a hydrogen atom, an alkoxycarbonyl group having 2 to 10 carbon atoms, an acyl group having 2 to 10 carbon atoms or a cycloalkylcarbonyl group having 4 to 10 carbon atoms; and R represents a halogen atom, an alkyl group having 1 to 4 carbon atoms or an alkoxy group having 1 to 4 carbon atoms, which is useful as a synthetic intermediate of an antiplatelet medicine and an elastase inhibitor, etc., and a process for preparing the same.

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