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    PROCESS FOR PREPARING CEPHALOSPORIN ANTIBIOTICS
    11.
    发明授权
    PROCESS FOR PREPARING CEPHALOSPORIN ANTIBIOTICS 失效

    公开(公告)号：KR830001543B1

    公开(公告)日：1983-08-10

    申请号：KR770000335

    申请日：1977-02-15

    Applicant: GLAXO LAB LTD

    Inventor： GREGSON MICHAEL ,  SYKES RICHARD BROOK

    IPC: C07D501/34

    Abstract: Cefuroxim esters I(R1 = C1-4 primary or secondary alkyl; R2 = C1-6 primary of secondary alkyl) were prepd. by the reaction of cefuroxim K salf with R2CHBrO2CR1 and the acylation of III with (Z)-2-(fur-2-y1)-2-methoxyimino-acetic acid. Thus, 4.57g cefuroxim was stirred with 760mg K2CO3 and 25ml N,N-dimethylformamide followed by the addn. of AcOCH2Br to give (R and S)-1-acetoxyethyl(6R,7R)-3-carbamoyloxymethyl-7-≮(Z)-2-(fur-2-y1)-2-methoxyiminoacetamido≉ceph-3-em-4-carboxylated. I are useful as antibiotics and are more easily absorbed after oral administration than cefuroxim.

    PROCESS FOR PREPARING SEMI-SYNTHETIC PENICILLINS
    12.
    发明授权
    PROCESS FOR PREPARING SEMI-SYNTHETIC PENICILLINS 失效

    公开(公告)号：KR810001202B1

    公开(公告)日：1981-09-28

    申请号：KR770000066

    申请日：1977-01-13

    Applicant: GLAXO LAB LTD

    Inventor： COTTI G ,  CROCI M

    IPC: C07D499/12

    Abstract: 6-Acylaminopenicillanic acid antibiotics having > 98 % purity was prepd. Thus, 6-Aminopenicillanic acid was treated with a silating agent, R1R2NCOR3 [R1 = H 1-6C alkyl or aralkyl; R2 = tri(1-6C) alkylsylyl or triarylsylyl; R3 = 1-6C alkyl, aralkyl [or R1N=C(OR2)R3[R1 = 1-6C alkyl, aralkyl, tri(1-6C)alkyl sylyl, triarylsylyl and the silayted deriv. I [R4 = H, tri(1-6C) alkylsylyl, triarylsylyl; R5 = tri(1-6C)alkylsylyl, triarylsylyl reacted with an acid chloride or protected acid chloride decompositing the sylyl group to yield the 6-acylaminopenicillanic acid.

    PROCESS FOR PREPARATION OF CEPHALOSPORIN COMPOUNDS
    13.
    发明授权
    PROCESS FOR PREPARATION OF CEPHALOSPORIN COMPOUNDS 失效

    公开(公告)号：KR790000420B1

    公开(公告)日：1979-05-14

    申请号：KR740004319

    申请日：1974-12-20

    Applicant: GLAXO LAB LTD

    Inventor： JANICE BRADSHAW ,  COOK M CH

    Abstract: Non-toxic 7- acylamidoceph-3 em -4-carboxylic acid derivs. (I; R= thienyl, furyl, Ra=Rb=H, C1-4 alkyl, C2-4 alkenyl, C3-7 cycloalkyl, phenyl, thienyl, furyl, carboxy, C2-5 alkoxycarbonyl, cyano) of syn-isomer or syn-and anti-mixt. contg. >90% syn-isomer were manufd. Acylation for I was carried out at -20-30≦̸C in the reactive media such as methylene chloride, dimethlformamide or acetonitril. I showed broad spectral action, esp. to gram-negative bacteria.

    Process for preparing 17{60 -monoesters of 17{60 , 21-dihydroxy-20-oxo steroids
    15.
    发明授权
    Process for preparing 17{60 -monoesters of 17{60 , 21-dihydroxy-20-oxo steroids 失效
    制备17种{60-21-二羟基-20-氧代甾族化合物的17- {

    公开(公告)号：US3891631A

    公开(公告)日：1975-06-24

    申请号：US38748773

    申请日：1973-08-10

    Applicant: GLAXO LAB LTD

    Inventor： PHILLIPPS GORDON HANLEY ,  BAIN BRIAN MACDONALD ,  DURRANT GRAHAM

    IPC: C07J5/00 ,  C07F1/00 ,  C07F1/08 ,  C07F9/08 ,  C07J7/00 ,  C07C173/00

    CPC classification number: C07F1/005 ,  C07F1/08 ,  C07F9/08

    Abstract: The specification describes a process for preparing 17 Alpha carboxylate or neutral phosphate or carbonate esters of 17 Alpha -21-dihydroxy-20-oxo steroids wherein a 21-carboxylate or neutral phosphate or carbonate ester of a 17 Alpha ,21-dihydroxy-20-oxosteroid is treated with a non-hydroxylic base in an anhydrous aprotic medium to remove a proton selectively from the 17 Alpha hydroxyl grouping, and the reaction mixture neutralised or acidified whereby the intermediate product is protonated. The base used in the process can be for example a carbanionoid e.g. alkali metal alkyl, or metal amide, e.g. alkali metal amide, base. The process is applicable to the preparation of a wide variety of 17-esters of the above-mentioned type. The process can also be used to prepare certain enol-aldehydes corresponding to the above-described 17-ester, a particular class of these enolaldehydes being described in the specification as novel compounds.

    Abstract translation: 该说明书描述了制备17α-二羟基-20-氧代甾族化合物的17α-羧酸酯或中性磷酸酯或碳酸酯的方法，其中17α，21-二羟基-20-氧代甾族化合物的21-羧酸酯或中性磷酸酯或碳酸酯 - 氧 - 类固醇在无水非质子介质中用非羟基碱处理以从17α-羟基选择性除去质子，并将反应混合物中和或酸化，由此中间产物被质子化。 在该方法中使用的碱可以是例如碳阴离子例如 碱金属烷基或金属酰胺，例如。 碱金属酰胺，碱。 该方法适用于制备上述类型的各种17-酯。 该方法也可用于制备对应于上述17-酯的某些烯醛，这些烯醇 - 醛的特定类别在本说明书中描述为新化合物。

    Novel 3{60 -hydroxysteroids of the 5{60 -pregnane series
    16.
    发明授权
    Novel 3{60 -hydroxysteroids of the 5{60 -pregnane series 失效
    5 {60-孕烷系列的新型3 {60-羟基类固醇

    公开(公告)号：US3883569A

    公开(公告)日：1975-05-13

    申请号：US20898571

    申请日：1971-12-16

    Applicant: GLAXO LAB LTD

    Inventor： PHILLIPPS GORDON HANLEY ,  NEWALL CHRISTOPHER EARLE ,  COOK MARTIN CHRISTOPHER

    IPC: A61K20060101 ,  C07C20060101 ,  C07C169/32

    CPC classification number: C07J5/00

    Abstract: Steroids of the 5 Alpha -pregnane series possessing a 3 Alpha hydroxy group, a 10-hydrogen atom or methyl group, an 11-oxo group, a 17 Alpha -hydrogen atom, a 20-oxo group, and a group of the formula -XR at the 21-position wherein -XR represents -OCOR, -OCOOR, -CCOSR or -OCONHR and R represents (a) a solubilising group containing a basic nitrogen atom, (b) a nitrobenzyl group (c) a lower alkyl group (when X is not -OCO-) or (d) a halogenoalkyl group. The steroids possess anaesthetic properties.

    Abstract translation: 具有3α-羟基，10-氢原子或甲基，11-氧代基，17α-氢原子，20-氧代基和式 - 基团的5α-孕烷系的类固醇 -XR为21位，其中-XR表示-OCOR，-OCOOR，-CCOSR或-OCONHR，R表示（a）含有碱性氮原子的增溶基团，（b）硝基苄基（c）低级烷基 （当X不为-OCO-）或（d）卤代烷基时。

    Preparation of 7-amino cephalosporin compound
    17.
    发明授权
    Preparation of 7-amino cephalosporin compound 失效
    制备7-氨基头孢菌素化合物

    公开(公告)号：US3882108A

    公开(公告)日：1975-05-06

    申请号：US24108772

    申请日：1972-04-04

    Applicant: GLAXO LAB LTD

    Inventor： CHAPMAN PHILIP HOWARD ,  HILLIGAN JAMES RAYMOND

    IPC: C07D20060101 ,  C07D501/04 ,  C07D501/18 ,  C07D501/60 ,  C07D99/24

    CPC classification number: C07D501/18

    Abstract: A process for preparing a 7-aminocephalosporin from a 7 Beta acylamidocephalosporin by the imide halide technique in which the 4-carboxyl group of the 7 Beta -acylamido cephalosporin is first protected by reaction with a phosphorus trihalide, particularly phosphorus trichloride.

    Abstract translation: 通过酰亚胺卤化物技术从7β-酰胺基头孢菌素制备7-氨基头孢菌素的方法，其中7β-酰氨基头孢菌素的4-羧基首先通过与三卤化磷，特别是三氯化磷的反应来保护。

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