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公开(公告)号:YU32937B
公开(公告)日:1975-12-31
申请号:YU229668
申请日:1968-10-02
Applicant: BAYER AG
Inventor: LEY K , METZGER K , FRITSCHE D , EHOLZER U , NAST R
IPC: C07D241/52 , C07D51/78
Abstract: 1,235,869. Quinoxaline-1,4-dioxides. FARBENFABRIKEN BAYER A.G. 3 Oct., 1968 [4 Oct., 1967], No. 47013/68. Heading C2C. Novel quinoxaline-1,4-dioxides of the Formula I in which R 1 is H, C 1-4 alkyl, C 1-4 alkoxy, or Cl, R 2 is straight or branched chain alkyl radical which may be substituted by OH, C 1-5 alkoxy, carbalkoxy, or dialkylamino (which term includes saturated N-containing heterocyclic radicals, R 3 is H, straight or branched chain alkyl radical which may be substituted by OH 2 C 1-5 alkoxy, carbalkoxy, mono- or di-alkylamino or when R 3 is H, R 2 may be cyclohexyl or R 2 and R 3 together with the amide nitrogen atom may form part of a 5- or 6-membered ring are prepared by reacting the appropriate benzofuroxane with an acetoacetic acid amide of the formula in the presence of ammonia or a primary amine in an organic solvent at a temperature of 20 to 100 C. or by oxidizing with hydrogen peroxide a quinoxaline derivative of the Formula XXIII above in which X is a radical readily convertible into a COOH or CON(R 2 )R 3 , group in the presence of glacial acetic acid or acetic anhydride, or an organic per-acid or mixture thereof and converting the thus obtained 1,4-dioxide to a compound of Formula I above. Pharmaceutical compositions having antibacterial activity and suitable for oral or parenteral administration, contain the above novel compounds in admixture with a solid or liquid diluents or carriers.
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公开(公告)号:YU229868A
公开(公告)日:1975-06-30
申请号:YU229868
申请日:1968-10-02
Applicant: BAYER AG
Inventor: LEO K , METZGER K , FRITSCHE D , EHOLZER U , NAST R
IPC: C07D241/52 , C07C153/03
Abstract: 2-Isothiouronium-methyl-3-carboxylic acid-amidoquinoxaline-1,4-di-N-oxide halides of the formula:
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公开(公告)号:BR6802856D0
公开(公告)日:1973-02-22
申请号:BR20285668
申请日:1968-10-04
Applicant: BAYER AG
Inventor: LEY K , EHOLZER U , NAST R , METZGER K , FRITSCHE D
IPC: C07D241/52
Abstract: 2-Isothiouronium-methyl-3-carboxylic acid-amidoquinoxaline-1,4-di-N-oxide halides of the formula:
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公开(公告)号:BR6802855D0
公开(公告)日:1973-02-22
申请号:BR20285568
申请日:1968-10-04
Applicant: BAYER AG
Inventor: LEY K , METZGER K , FRITSCHE D , EHOLZER U , NAST R
IPC: C07D241/52
Abstract: 1,235,869. Quinoxaline-1,4-dioxides. FARBENFABRIKEN BAYER A.G. 3 Oct., 1968 [4 Oct., 1967], No. 47013/68. Heading C2C. Novel quinoxaline-1,4-dioxides of the Formula I in which R 1 is H, C 1-4 alkyl, C 1-4 alkoxy, or Cl, R 2 is straight or branched chain alkyl radical which may be substituted by OH, C 1-5 alkoxy, carbalkoxy, or dialkylamino (which term includes saturated N-containing heterocyclic radicals, R 3 is H, straight or branched chain alkyl radical which may be substituted by OH 2 C 1-5 alkoxy, carbalkoxy, mono- or di-alkylamino or when R 3 is H, R 2 may be cyclohexyl or R 2 and R 3 together with the amide nitrogen atom may form part of a 5- or 6-membered ring are prepared by reacting the appropriate benzofuroxane with an acetoacetic acid amide of the formula in the presence of ammonia or a primary amine in an organic solvent at a temperature of 20 to 100 C. or by oxidizing with hydrogen peroxide a quinoxaline derivative of the Formula XXIII above in which X is a radical readily convertible into a COOH or CON(R 2 )R 3 , group in the presence of glacial acetic acid or acetic anhydride, or an organic per-acid or mixture thereof and converting the thus obtained 1,4-dioxide to a compound of Formula I above. Pharmaceutical compositions having antibacterial activity and suitable for oral or parenteral administration, contain the above novel compounds in admixture with a solid or liquid diluents or carriers.
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