WERKWIJZE VOOR HET BEREIDEN VAN 3'-DESOXYDERIVATEN VAN AMINOGLYCOSIDE ANTIBIOTICA, ALSMEDE WERKWIJZE VOOR HET BEREIDEN VAN EEN FARMACEUTISCH PREPARAAT, WAARIN EEN DERGELIJKE VERBINDING ALS ACTIEVE STOF AANWEZIG IS.

摘要

1426910 Aminoglycoside antibiotics ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI 30 Nov 1973 [8 Dec 1972] 55685/73 Heading C2C The invention comprises 31-deoxy-vistamycin, its 61-N-C 1-4 -alkyl derivatives, the 31-deoxy-61- N-C 1-4 -alkyl derivatives of neamine and kanamycin B, and their pharmaceutically acceptable acid addition salts. In examples, these compounds, 31 - deoxy - neamine and 31 - deoxy kanamycin B are prepared by protecting all of the amino groups in kanamycin B, neamine or vistamycin, thus forming corresponding polycarbamates, poly - arylimines or poly - benzamides, and some of the OH groups by forming cyclic ketals (in which unprotected OH groups may be esterified), then forming a corresponding 31 - tosylate or mesylate (in which a further OH group may be simultaneously tosylated or mesylated), and reacting these sulphonates with alkali metal, bromide or iodide giving the 31- bromo- or 31 - iodo - 31 - deoxy compounds which are reduced to the desired compounds, the protecting group being generally removed in a final step; 31-deoxy-61-N-methyl derivatives are made by reducing the corresponding 31- deoxy - 61 - N - benzylory compounds and purifying the desired products by means of intermediate poly - anisylimino - 31 - deoxy - 61- N-methyl derivatives. Therapeutic compositions for oral, parenteral or topical administration comprise the new compounds, which are active against grampositive and gram-negative bacteria.