PROCESS FOR PREPARING CEPHEM DERIVATIVES

    公开(公告)号:KR810000981B1

    公开(公告)日:1981-08-25

    申请号:KR780000611

    申请日:1978-03-09

    Applicant: HOECHST AG

    Abstract: Title compds. [I; R1 = H, lower alkoxy; R2=H, alkyl, phthalide; X = O, S, Me; A = H, alkoxy, halogen, CH2Y(Y = H, acyloxy, alkoxy, carbamoyloxy, or acyl, alkyl, 5-6membered heterocyclic compd. -substituted thionyl group) were prepd. by reaction of II and III, and removing protected-group of amino from IV. Thus, III(R = 2-triphenylmethyl) in MeCl, Et3N and pivaloylchloride were mixed and reacted with II(R1,R2,A = H) and Et3N to give IV(R = 2-triphenylmethyl; R1,R2,A = H). IV was reacted with formic acid to give yellow crystal-form I.

    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.

    Acylaminopenicillanic acids and salts thereof
    3.
    发明授权
    Acylaminopenicillanic acids and salts thereof 失效
    ACYLAMINOPENICILLANIC酸及其盐

    公开(公告)号:US3749711A

    公开(公告)日:1973-07-31

    申请号:US3749711D

    申请日:1970-09-18

    Applicant: HOECHST AG

    CPC classification number: C07D499/00 C07D233/22

    Abstract: ANTIBIOTICALLY ACTIVE ACYLAMINOPENICILLANIC ACIDS OF THE GENERAL FORMULA I

    6-(R1-N=C(-N(-R2)(-R3))-A-B-CH2-CO-NH-),2-(HOOC-),3,3-

    DI(CH3-)PENAM

    IN WHICH R1, R2 AND R3 REPRESENT HYDROGEN OR LOWER ALKYL GROUPS, R1 AND R2 MAY FORM TOGETHER AN ALKYLENE GROUP WHICH MAY BE SUBSTITUTED, A REPRESENTS A PHENYLENE OR THIENYLENE GROUP WHICH MAY BE SUBSTITUTED AND B REPRESENTS OXYGEN OR A CHEMICAL BOND, AND THE PHYSIOLOGICALLY TOLERATED SALTS THEREOF, PHARMACEUTICAL PREPARATIONS CONTAINING THESE COMPOUNDS AND PROCESS FOR THE PREPARATION OF SUCH COMPOUNDS AND PREPARATIONS.

    7.
    发明专利
    未知

    公开(公告)号:SE7804185L

    公开(公告)日:1978-10-16

    申请号:SE7804185

    申请日:1978-04-13

    Applicant: HOECHST AG

    Abstract: What are disclosed are cephem compounds of the formula in which R1 denotes hydrogen, an optionally substituted alkyl, acyl, arylsulfonyl or alkylsulfonyl group or an amino-protective group which is known from peptide chemistry, R2 denotes hydrogen or an optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, aralkyl, acyl, aryl, arylsulfonyl, alkylsulfonyl or heterocyclic group, R3 denotes hydrogen, an ester group or a cation, R4 denotes hydrogen, a lower alkoxy group or a group which can be converted to this, X denotes a SO group in the R or S configuration or a SO2 group and A denotes hydrogen, an optionally substituted alkoxy or alkenyloxy group, halogen or a group -CH2Y, in which Y represents hydrogen, halogen or the radical of a nucleophilic compound, and in which the R2O group is in the syn-position, which compounds are valuable chemotherapeutic agents having a very powerful antimicrobial action against Gram-positive and Gram-negative bacteria and an unexpectedly good action against penicillinase-forming Staphilococci.

    8.
    发明专利
    未知

    公开(公告)号:DK162878A

    公开(公告)日:1978-10-16

    申请号:DK162878

    申请日:1978-04-14

    Applicant: HOECHST AG

    Abstract: What are disclosed are cephem compounds of the formula in which R1 denotes hydrogen, an optionally substituted alkyl, acyl, arylsulfonyl or alkylsulfonyl group or an amino-protective group which is known from peptide chemistry, R2 denotes hydrogen or an optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, aralkyl, acyl, aryl, arylsulfonyl, alkylsulfonyl or heterocyclic group, R3 denotes hydrogen, an ester group or a cation, R4 denotes hydrogen, a lower alkoxy group or a group which can be converted to this, X denotes a SO group in the R or S configuration or a SO2 group and A denotes hydrogen, an optionally substituted alkoxy or alkenyloxy group, halogen or a group -CH2Y, in which Y represents hydrogen, halogen or the radical of a nucleophilic compound, and in which the R2O group is in the syn-position, which compounds are valuable chemotherapeutic agents having a very powerful antimicrobial action against Gram-positive and Gram-negative bacteria and an unexpectedly good action against penicillinase-forming Staphilococci.

    9.
    发明专利
    未知

    公开(公告)号:NO754232L

    公开(公告)日:1976-06-15

    申请号:NO754232

    申请日:1975-12-12

    Applicant: HOECHST AG

    Abstract: Acylaminopenicillanic acids of the general formula in which R1, R2 and R3 represent hydrogen or lower alkyl which may be substituted, and in which the radicals R1 and R2 or R2 and R3 may form together an alkylene radical which may be substituted, R4 and R5 represent hydrogen or lower alkyl, R6 represents phenyl which may be substituted, a monocyclic aromatic heterocycle which may be substituted, or dihydrophenyl, A represents a benzene or thiophene ring which may be substituted, and X represents oxygen or a single bond, a process for preparing them and pharmaceutical compositions active against bacterial infections containing these compounds.

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