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    IMPROVEMENT OF PENICILIN PREPARATION
    1.
    发明授权
    IMPROVEMENT OF PENICILIN PREPARATION 失效

    公开(公告)号：KR790000925B1

    公开(公告)日：1979-07-31

    申请号：KR750000994

    申请日：1975-05-08

    Applicant: GLAXO LAB LTD

    Inventor： MARTIN G D ,  COWLEY B R

    Abstract: α-Aminoacylpenicillins were manufd. from 6-aminopenicillanic acid (6-APA) by a modified method. The suspension of 6-APA in chlorinated hydrocarbon solvent contg. PH 10 tri(low alkyl) amine was dissolved by stirring for 1hr at 25≦̸C and neutralized with N,N-dimethylacetamide HCl at 0≦̸C. The neutralized soln. was contacted to org. solvent dissolving the anhydride mix. of low alkoxy formic acid and N-protected deriv. of amino acid to give α-aminoacylpenicillins.

    PROCESS FOR PREPARING CLAVURANIC ACID DERIVATIVES
    3.
    发明授权
    PROCESS FOR PREPARING CLAVURANIC ACID DERIVATIVES 失效

    公开(公告)号：KR810001655B1

    公开(公告)日：1981-10-27

    申请号：KR770002451

    申请日：1977-10-24

    Applicant: GLAXO LAB LTD

    Inventor： TONGE ALAN P ,  CHERRY PETER C ,  NEWALL CHRISTOPHER E

    IPC: C07D498/04

    Abstract: Clavuranic acid derivs. (I; R = acyl amino group; R1 = carboxy1, esterified carboxy1 group), useful as antibiotic, were prepd. by reacting compd. (II) with acylating agent. Thus, acetone 5 ml and anhydrous acetic acid 0.58 g soln. was added in the 50% acetone 45ml soln. of NaHCO3 96 g and Acc 0.90 g for 10 min, stirred for 30 min and then poured in the saturated brine 50 ml. The soln. was extracted with ethyl - acetate after adjusting the pH to 3-4. The extract was dried, added in the ethyl acetate soln. of sodium 2-ethylhexanoate 0.35 g soln., and then stirred for 15 min. The obtained solid material was washed with ether to give compd. (I).

    PROCESS FOR PREPARING SEMI-SYNTHETIC PENICILLIN ANTIBIOTICS
    5.
    发明授权
    PROCESS FOR PREPARING SEMI-SYNTHETIC PENICILLIN ANTIBIOTICS 失效

    公开(公告)号：KR810000856B1

    公开(公告)日：1981-08-10

    申请号：KR770000065

    申请日：1977-01-13

    Applicant: GLAXO LAB LTD

    Inventor： CROCI M ,  COTTI G

    IPC: C07D499/12

    Abstract: 6-Acylaminopenicillanic acid were prepared from 6-APA. Thus, mono- or di-silylated 6-aminopenicillanic acid were acylated with corresponding acid chloride in the presence of primary or secondary carboxamide [R'CONHR2; R1 = C1-6 alkyl, aralkyl as halogenated hydrogen acceptor and removing of silylated or other protected group was followed. By using above carboxamide such as acetamide, methylurea instead of dialkylaniline, trialkylamine, piperidine or pyridine, final products were obtained with high yield and low basic contamination related to toxicity.

    PROCESS FOR PREPARING CEPHALOSPORIN ANTIBIOTICS
    8.
    发明授权
    PROCESS FOR PREPARING CEPHALOSPORIN ANTIBIOTICS 失效

    公开(公告)号：KR830001521B1

    公开(公告)日：1983-08-08

    申请号：KR770000334

    申请日：1977-02-15

    Applicant: GLAXO LAB LTD

    Inventor： GREGSON MICHAEL ,  SYKES RICHARD BROOK

    IPC: C07D501/32

    Abstract: Cefuroxime alkanoyloxymethyl esters I (R = C1-4 alkyl) were prepd. for use as antibiotics. Thus, cefuroxime was stirred with K2CO3 and DMF, followed by the addn. of acetoxy methyl bromide to give I (R = CH3). I are more easily absorbed through the gastrointestinal tract than the parent cefuroxime and thus are suitable for oral administraction.

    PROCESS FOR THE PURIFICATION OF CLAVULANIC ACID
    9.
    发明授权
    PROCESS FOR THE PURIFICATION OF CLAVULANIC ACID 失效

    公开(公告)号：KR800001241B1

    公开(公告)日：1980-10-25

    申请号：KR760000291

    申请日：1976-02-06

    Applicant: GLAXO LAB LTD

    Inventor： NOBLE D ,  WALL W ,  NOBLE H

    IPC: C07D498/04

    Abstract: Title compd. (I) useful as antibiotics, and its salts were prepd. from the culture filtrate of Streptomyces clavuligerus NRRL 3585. Thus, 25l inoculum grown on a complex medium was mixed with 475l of a medium contg. soybean meal 3.0, FeSO47H2O 0.01, K2HPO40.01, sol. starch 4.7%, and silicon antifoaming agent 0.05% and cultured in 700l fermentor for 2 hr at 28≦̸C and pH 6.5 with agitation and aeration at 0.56 v/v/min. The culture filtrate was decolorized with active C, the column washed with 90l water, and I eluted with 180l of 60% acetone.

    PROCESS FOR PREPARATION OF CEPHALOSPORIN ANTIBIOTICS
    10.
    发明授权
    PROCESS FOR PREPARATION OF CEPHALOSPORIN ANTIBIOTICS 失效

    公开(公告)号：KR790001651B1

    公开(公告)日：1979-12-01

    申请号：KR790003428

    申请日：1979-10-06

    Applicant: GLAXO LAB LTD

    Inventor： MARTIN CHRISTOPHER COOK ,  JANICE BRADSHAW ,  GORDON IAN GREGORY

    IPC: C07D501/60

    Abstract: Cephalosporin antibiotics (I;R1 = furyl, thienyl, phenyl; R2 = C1-4 alkyl, C3-7 cycloalkyl, or phenyl) and its non-toxic derivs. were prepd. by treating compd. (II; R11 = H carboxyl protecting group) with carbamoyl group forming agent followed by elimination of carbamoyl protecting group or N-protected group. The carbamoyl group forming agent is forming carbamoyl oxymethyl group or N-protected carbamoyloxymethyl group at 3-position.

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