Drug – bio-affecting and body treating compositions – Conjugate or complex of monoclonal or polyclonal antibody,... – Conjugated via claimed linking group – bond – chelating agent,...
Patent
1982-01-08
1984-03-27
Brown, Johnnie R.
Drug, bio-affecting and body treating compositions
Conjugate or complex of monoclonal or polyclonal antibody,...
Conjugated via claimed linking group, bond, chelating agent,...
424180, 435 74, 435172, 435253, 536 72, 549264, 549271, A61K 3171, C07D31300, C07H 1708, C12P 1962
Patent
active
044394268
ABSTRACT:
From the fermentation carried, out with mutants blocked in the synthesis respectively of erythromycin and of oleandomycin, namely Streptomyces erythreus ATCC 31772 and Streptomyces antibioticus ATCC 31771, using as the substrate a derivative of erythronolide A, namely (8S)-8-fluoroerythronolide A, a derivative of erythronolide B, namely (8S)-8-fluoroerythronolide B, or a derivative of 3-O-mycarosyl-erythronolide B, namely 3-O-mycarosyl-(8S)-fluoroerythronolide B, the corresponding (8S)-8-fluoro derivatives of the erythromycins A, B, C and D, as well as 3-O-oleandrosyl-5-desosaminyl-(8S)-8-fluoroerythronolide A and 3-O-oleandrosyl-5-O-desosaminyl-(8S)-8-fluoroerythronolide B, all belonging to the class of the macrolide antibiotics are obtained.
The preparation of the aforesaid substrate comprises the convention of erythronolide A, erythronolide B or 3-O-mycarosyl-erythronolide B into the corresponding hermiacetal, the reaction of the latter with a compound capable of generating electrophlic fluorine and the opening of the resulting acetal with aqueous acid.
REFERENCES:
patent: 3697547 (1972-10-01), Kurath et al.
patent: 3780019 (1973-12-01), Wildsmith
patent: 3816397 (1974-06-01), Tadanier et al.
patent: 3855200 (1974-12-01), Krowicki et al.
Bright, "Chem. Abst.", vol. 90, 1979, p. 152552(c).
Adachi et al., "Chem. Abst.", vol. 90, 1979, p. 152554(e).
Cappelletti Leonardo M.
Toscano Luciano
Brown Johnnie R.
Pierrel S.p.A.
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