PROCESS FOR PREPARATION OF TETRAHYDRO ACRIDONES

    公开(公告)号:KR790000398B1

    公开(公告)日:1979-05-11

    申请号:KR740003254

    申请日:1974-08-01

    Applicant: HOECHST AG

    Abstract: Tetrahydroacridones (R' = O or -N -NH2, R2 = R3 =R4 =R5 =R6 = R7 = phenyl substituted for H, C1-C4 alkyl, F, Cl, Br, I, trifluoromethly, NO2, CN, carbamyl, sulfamyl, acetyl, lower alkyl-sulfoxy and phenyl-sulfoxy, R8-R11 = H, F, Cl, Br, I trifluoromethyl, cyano, lower alkyl, lower alkoxy, R12 = H, OH, lower acyloxy), useful as antimalarial and coccidostatic, were prepd. by condensing nitrobenzaldehyde (II) with cyclohexadienones (III) in the hydrophilic org. solvent in the presense of inorg. acid.

    PROCESS FOR PREPARING CEPHALOSPORIN DERIVATIVES

    公开(公告)号:KR820001127B1

    公开(公告)日:1982-06-26

    申请号:KR780003624

    申请日:1978-11-30

    Applicant: HOECHST AG

    Abstract: Title compds. (I; n = 0-1; X = H, C1-4 alkyl, carboxymethyl, C1-4 alkoxycarbonylmethyl, cyanomethyl; Y = Me, halogen; A = H, ester, cation) were prepd. from IV (R1 = H, amino protecting group; X1 = X or -CH2CO2R3; R3 = separating group) obtained by reaction of II and III. Thus, 980 mg 7-≮αsyn-methoxyimino-α-(2-amino-5-chloro-thiazol-4-yl)-acetamido≉-cephalosporanic acid was dissolved in a mixed soln. contg. 8 ml 98% formic acid and 2 ml methanol, added 410 mg THF soln. contg. 85% m-chloroperbenzoic acid, and stirred for 1 hr to give 850 mg I.

    ANTIMALARIAL COMPOSITIONS CONTAINING A TETRAHYDROACRIDONE AND ANOTHER COMPOUND

    公开(公告)号:NZ188740A

    公开(公告)日:1980-11-28

    申请号:NZ18874078

    申请日:1978-10-26

    Applicant: HOECHST AG

    Abstract: Antimalarial compositions are disclosed containing as the active ingredient a mixture of a tetrahydroacridone of the general formula I in which R1 represents methyl, phenyl, p-chlorophenyl, m-chlorophenyl, p-fluorophenyl, p-trifluoromethylphenyl, o-trifluoromethylphenyl or o-chloro-p-trifluoromethylphenyl, R2 represents hydrogen or methyl, and R3 represents fluorine or chlorine, or a salt of such a compound with a physiologically compatible acid or base, with (a) 6-methoxy- alpha -(5-vinyl-2-quinuclidinyl)-4-quinoline-methanol (Quinine), (b) 7-chloro-4-(diethylamino-1-methyl-butylamino)-quinoline (Chloroquine), (c) alpha -(2-piperidyl)-2,8-bis(trifluoromethyl)-4-quinolinemethanol (Mefloquine), (d) 8-(4-amino-1-methylbutylamino)-6-methoxy-quinoline (Primaquine), (e) 2,4-diamino-5-p-chlorophenyl-6-ethylpyrimidine (Pyrimethamine), (f) 4,6-diamino-1-(p-chlorophenyl)-1,2-dihydro-2,2-dimethyl-s-triazine (Cycloguanil), (g) 2,4-diamino-5-(3,4,5-trimethoxybenzyl)-pyrimidine (Trimethoprim), (h) N'-(5,6-dimethoxy-4-pyrimidyl)-sulfanilamide (Sulfadoxine), or (i) 4,4'-diaminodiphenylsulfone (Dapsone), or with a salt of a compound sub (a) to (i), with a physiologically compatible acid or base, the mixtures being in a proportion by weight of between 25:1 and 1:300 (tetrahydroacridone to compound sub (a) to (i)) in admixture with a pharmaceutically acceptable carrier and/or adjuvant.

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