Merck Patent Gesellschaft MIT Beschrankter Haftung

Merck Patent Gesellschaft MIT Beschraenkter Haftung

Richard Kirchlechner

Helmut Wahlig

Werner Rogalski

Rudolf Gottschlich

Rolf Bergmann

Joachim Gante

Dieter Orth

Elvira Dingeldein

Michael Casutt

Jurgen Seubert

Arno Basedow

Rosmarie Steinigeweg

Walter Hameister

Juergen Seubert

Process for the preparation of 5-membered nitrogen containing

Flavonoid phosphates of aminoglycoside antibiotics are useful sparingly soluble salts, e.g., for achieving a depot effect.

Flavonoid phosphate salts of aminoglycoside antibiotics

A process for the preparation of racemic 6-thiatetracycline derivatives comprises treating a mixture of epimers of corresponding 1,4,4a,5,5a,6,11,12a-octahydro-3,12-dihydroxy-1,11-dioxo-6-thianaphthacene -2-carboxamides with a saturated heterocyclic secondary amine having a total of 4 to 12 carbon atoms for a sufficient length of time at temperatures of about 15.degree.-120.degree. C.

Process for the preparation of sterically uniform, natural

Tetracyclic compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each are H or alkyl, R.sup.5 is H, F, Cl, Br, CF.sub.3, OH, alkyl, alkoxy, NO.sub.2, NH.sub.2, alkylamino, dialkylamino or acylamino and X is O, S, SO, SO.sub.2, NH, N-alkyl or N-acyl, alkyl and alkoxy in each case being of 1-3 carbon atoms and acyl in each case being of 1-4 carbon atoms, with the proviso that when R.sup.5 is methoxy and X is a sulfur atom, R.sup.5 is in the 8- or 9-position only, and their physiologically acceptable acid addition salts, possess broad spectrum antibacterial activity, including tetracycline-resistant Gram-positive and Gram-negative organisms.

Tetracyclic compounds

7-Methoxy-6-thiatetracyclines of the formula ##SPC1## Wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each are H or alkyl of 1 to 4 carbon atoms, and the physiologically acceptable acid addition salts thereof.

7-Methoxy-6-thiatetracyclines and their preparation

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Darmstadt, Germany

Richard Kirchlechner