Alkanoic acid esters of 5-hydroxytetracycline and process for preparation
阅读：747发布：2022-08-15
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1. A COMPOUND SELECTED FROM THE GROUP CONSISTING OF 10,12A-(O,O-DIACYL)-5-HYDROXYTETRACYCLINE, THE ACID ADDITION SALTS, THE METAL SALTS, AND THE METAL SALT COMPLEXES THEREOF, EACH OF SAID ACYL GROUPS BEING OF THE FORMULA RCO- WHEREIN R IS AN ALKYL GROUP HAVING FROM 1 TO 5 CARBON ATOMS.
5. A PROCESS FOR THE PREPARATION OF 10,12A-(O,O-DIACYL)-5-HYDROXYTETRACYCLINE WHICH COMPRISES TREATING A MIXTURE OF ONE MOLEULAR PROPORTION OF AMPHOTERIC 5HYDROXYTETRACYCLINE AND FROM ABOUT 2 TO 8 MOLECULAR PROPORTIONS OF PYRIDINE WITH FROM ABOUT 2 TO 8 MOLECULAR PROPORTIONS OF AN ALKYL CARBOXYLIC ACID ANHYDRIDE HAVING THE FORMULA (RCO)2O WHEREIN R IS AN ALKYL GROUP HAVING FROM 1 TO 5 CARBON ATOMS AT A TEMPERATURE OF FROM ABOUT 15 TO 40*C.
8. THE PROCESS WHICH COMPRISES TREATING 10,12A(O,ODIACYL)-5-HYDROXYTETRACYCLINE WITH AN AQUEOUS SOLUTION CONTAINING AN APPROXIMATELY EQUIMOLECULAR PROPORTION OF AN ALKALI METAL HYDROXIDE AND APPROXIMATELY A 1/2 MOLAR PROPORTION OF A WATER SOLUBLE MAGNESIUM SALT AT A TEMPPERATURE OF ABOUT 15 TO 40*C. AND RECOVERING RESULTING 5,12A-DIESTER OF 5-HYDROXYTETRACYCLINE, SAID ACYL GROUPS BEING OF THE FORMULA RCO- WHEREIN R IN AN ALKYL GROUP HAVING 1 TO 5 CARBON ATOMS.
10. THE PROCESS WHICH COMPRISES TREATING 10,12-(O,ODIACYL)-5-HYDROXYTETRACYCLINE WITH AT LEAST A MOLAR EQUIVALENT OF AQUEOUS AMMONIA AT A TEMPERATURE OF FROM ABOUT 15 TO 40*C. FOR A PERIOD OF TIME JUST SUFFICIENT TO SELECTIVELY HYDROLYZE SAID 10-O-ACYL GROUP, SAID O-ACYL GROUPS BEING OF THE FORMULA RCO-WHEREIN R IN AN ALKYL GROUP HAVING FROM 1 TO 5 CARBON ATOMS.
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