SUM, PHAIK-ENG,HOW, DAVID BRIAN,HOPPER, DARRIN WILLIAM,VERA, MATTHEW DOUGLAS,SABATINI, JOSHUA JAMES
申请号：
ES09010915
公开号：
ES2372635T3
申请日:
2004.12.07
申请国别(地区):
ES
年份:
2012
代理人:
摘要：
A process for preparing a compound of the formula or a pharmaceutically acceptable salt thereof, in which: X is selected from hydrogen, amino, NR 11 R 12, alkyl of 1 to 12 carbon atoms substituted in form optionally, aryl of 6, 10 or 14 optionally substituted carbon atoms, optionally substituted vinyl, optionally substituted alkynyl of 2 to 12 carbon atoms and halogen； R 1 and R 2 are each independently H or alkyl of 1 to 12 carbon atoms or R 1 and R 2 when optionally taken together with the nitrogen atom to which each is attached form a saturated hydrocarbon ring of 3 7 members； R 11 and R 12 are each independently H or alkyl of 1 to 12 carbon atoms or R 11 and R 12 when optionally taken together with the nitrogen atom to which each is attached form a saturated hydrocarbon ring of 3 7 members； And hydrogen is selected, alkyl of 1 to 12 carbon atoms optionally substituted, aryl of 6, 10 or 14 carbon atoms optionally substituted, alkenyl of 2 to 12 carbon atoms optionally substituted, vinyl, alkynyl 2 to 12 carbon atoms optionally substituted and halogen； comprising one of the following: i) hydrolyzing a substituted amine of formula: in which the variables are those defined above, with acid to give a compound of formula and if it is desired to convert the product into a salt thereof acceptable from the point pharmaceutical view； or (ii) reacting a chlorine compound of formula: in which the variables are those defined above, with acid to give a substituted 9- (2-chloromethylcarbonylamino) -6-demethyl-6-deoxytetracycline of formula in which the variables are those defined above, followed by reacting 9- (2-chloromethylcarbonylamino) substituted-6-desmethyl-6-deoxytetracycline with an amine R 1 R 2 NH to give the compound of formula in which the variables are those defined above, and isolate the compound or a pharmaceutically acceptable salt thereof.Un procedimiento de preparación de un compuesto de fórmula o una sal del mismo aceptable desde el punto de vista farmacéuti
