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    4''-DEOXY-4''-OXOERYTHROMYCIN B DERIVATIVES
    17.
    发明专利
    4''-DEOXY-4''-OXOERYTHROMYCIN B DERIVATIVES 未知

    公开(公告)号：ZA743085B

    公开(公告)日：1975-05-28

    申请号：ZA743085

    申请日：1974-05-14

    Applicant: ABBOTT LAB

    Inventor： JONES P ,  PAUVLIK J ,  TADANIER J ,  MARTIN J ,  MCALPINE J

    IPC: C07H17/08 ,  C07C

    Abstract: 1463850 4 11 -Dioxy-4-oxo-erythromycin B derivatives ABBOTT LABORATORIES 19 June 1974 [21 June 1973] 27249/74 Heading C2C Novel compounds I and II in which R 5 is CH(R 7 )-SR 8 (where R 7 is hydrogen or C 1-6 alkyl and R 8 is C 1-6 alkyl) and R 6 is hydrogen or C 2-6 alkanoyl provided that when R 6 is hydrogen then R 5 is also hydrogen are prepared by reacting erythromycin B with a di-C 1-6 alkyl-sulphoxide and C 2-6 alkanoic acid anhydride to form a compound I (R 5 = CH(R 7 )-SR 8 and R 6 = C 2-6 alkanoyl) which is hydrolysed with an alkali metal bicarbonate to form a compound I (R 5 =CH(R 7 )-SR 8 and R 6 = hydrogen) which in the presence of HgO/ HgCl 2 forms a compound II which is hydrolysed by dil. HCl to compound I (R 5 = R 6 = hydrogen). Compound I (R 5 =R 6 =hydrogen) is also prepared by treating compound II with chloramine T.

    SULFONYL DERIVATIVES OF ERYTHROMYCIN
    18.
    发明专利
    SULFONYL DERIVATIVES OF ERYTHROMYCIN 未知

    公开(公告)号：ZA742272B

    公开(公告)日：1975-03-26

    申请号：ZA742272

    申请日：1974-04-09

    Applicant: ABBOTT LAB

    Inventor： TADANIER J ,  HALLAS R ,  MARTIN J

    IPC: A61K31/335 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/08 ,  C07C

    Abstract: 1467296 Erythromycin derivatives ABBOTT LABORATORIES 1 May 1974 [4 May 1973] 19163/74 Heading C2C Novel erythromycin derivatives of the general formula wherein R is a C 1-6 alkyl, C 2-6 alkenyl, or optionally nuclear substituted aryl, benzyl or aroxyalkyl group, R 1 is a hydrogen atom or methyl group, R 2 is a hydrogen atom or C 1-6 alkanoyl group and R 3 is a hydrogen atom or hydroxyl group, provided that R 1 and R 3 are not simultaneously a hydrogen atom and the nuclear substituent is nitro, alkyl or halogen are prepared by reacting the corresponding compound in which the -OSO 2 R group is replaced by -OH with RSO 2 Cl (when R is vinyl in the product, R may be 2-bromoethyl in the starting material), followed optionally by hydrolysis or alcoholysis when R 2 is a C 1-6 alkanoyl group to give the corresponding product wherein R 2 is a hydrogen atom. Pharmaceutical compositions having antibiotic activity comprise, as active ingredient, an erythromycin derivative of the above general formula, together with an appropriate carrier.

    10,11-ANHYDROERYTHROMYCINS
    19.
    发明专利
    10,11-ANHYDROERYTHROMYCINS 未知

    公开(公告)号：ZA733182B

    公开(公告)日：1974-04-24

    申请号：ZA733182

    申请日：1973-05-10

    Applicant: ABBOTT LAB

    Inventor： TADANIER J ,  MARTIN J

    IPC: C07H17/08

    Abstract: 1411454 Erythromycin derivatives ABBOTT LABORATORIES 5 June 1973 [15 June 1972] 26841/73 Heading C2C The invention comprises the novel antibiotics 10,11-anhydroerythromycin B, 10, 11- anhydroerythromycin B enol ether, 10,11- anhydroerythromycin A enol ether, 10,11- anhydroerythromycin A and 10,11-anhydroerythromycin A 6, 9:9,12-spiroketal. 10,11- Anhydroerythromycin A and B may be prepared by treating an 11-o-methanesulphonyl-2 1 -oacetyl.4 11 -o-formylerythromycin A or B with a strong, non-nucleophilic base in an inert solvent and subsequently with methanol. The strong, non-nucleophilic base may be 1,5-diazabicyclo- [5,4,0]-undecene-5, 1,5-diazabicyclo-[4,3,0]-nonene-5 or sodium carbonate. Alternatively, the 10,11-anhydroerythromycins A and B may be prepared by reacting an 11-o-methanesulphonyl erythromycin which does not contain the 2 1 - acetyl, 4 11 -formyl blocking groups with such a base. The 11-o-methanesulphonyl-2 1 -o-acetyl- 4 11 -o-formylerythromycins A and B are prepared in accordance with the method described in Specification 1,402,045. A mixture of 10,11- anhydroerythromycin A enol ether and 10,11- anhydroerythromycin A 6,9 : 9,12-spiroketal is prepared by treating 11,12-epoxyerythromycin A (prepared as described in Specification 1,402,046) with glacial acetic acid and allowing to stand for 48 hours. The 10,11-anhydroerythromycins A and B are converted to the corresponding enol ethers by treatment with glacial acetic acid.

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