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    PROCESS FOR PREPARATION OF CEPHALOSPORIN ANTIBIOTICS
    2.
    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.

    0-AZA-9-OXAFLUORENES
    7.
    发明专利
    0-AZA-9-OXAFLUORENES 未知

    公开(公告)号：GB1300928A

    公开(公告)日：1972-12-29

    申请号：GB2384069

    申请日：1969-05-09

    Applicant: GLAXO LAB LTD

    Inventor： JOHN DEREK COCKER ,  GORDON IAN GREGORY

    IPC: C07D213/64 ,  C07D213/643 ,  C07D213/73 ,  C07D491/048

    Abstract: 1300928 1-Aza-9-oxafluorenes GLAXO LABORATORIES Ltd 30 April 1970 [9 May 1969] 23840/69 Heading C2C [Also in Division A5] Novel 1-aza-9-oxafluorenes are prepared (a) by cyclization of a 2-phenoxy-pyridine-3- diazonium salt (which is unsubstituted in an o-position of the phenoxy group) using a catalyst or by photolysis; (b) by photolysis of a 2-(2 1 -halophenoxy)-pyridine or a 2-phenoxypyridine-2 1 -diazonium salt (which is unsubstituted in the 3-position of the pyridine ring); (c) when a nucleophilic residue is present at the 2- and/or 4-position, by reaction of a 2- and/or 4-halo-1-aza-9-oxafluorene with a nucleophilic reagent; (d) when a nucleophilic residue is present at the 2-position, by reaction of a 2- unsubstituted 1-OR 3 -1-aza-9-oxafluorene quaternary salt, wherein R 3 is an aliphatic or araliphatic group, with a nucleophilic reagent; (e) when an oxygen atom is attached to the ring nitrogen atom, by reaction of a 1-aza-9-oxafluorene with an organic or inorganic peracid; (f) when a 6-substituent is present, by direct electrophilic substitution of the corresponding 6-unsubstituted compound; (g) when the starting material for process (d) above is required, by reaction of the corresponding N-oxide with an aliphatic or araliphatic reactive ester; and (h) when a 4-halo substituent is present, by reaction of a 4-unsubstituted 1-aza-9-oxafluorene-1- oxide with a phosphorus oxyhalide. 2 - Phenoxy - pyridine - 3 - diazonium salts (which are unsubstituted in an o-position of the phenoxy group) are prepared by condensation of a phenol having a free o-position with a 2- halo-3-nitropyridine, reduction of the resulting 2-phenoxy-3-nitropyridine and diazotization of the 2 - phenoxy - 3 - aminopyridine so obtained. 2-(o-Chlorophenoxy)-pyridine is prepared by reaction of o-chlorophenol with 2-chloropyridine in the presence of potassium hydroxide.

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