SALAET FERRE, Josep,MARQUILLAS OLONDRIZ, Francisco
申请号：
ES13780107
公开号：
ES2625417T3
申请日:
2013.10.16
申请国别(地区):
ES
年份:
2017
代理人:
摘要：
A process for preparing a compound of formula (IV): ** Formula ** where L is (a) 1H-imidazol-1-yl, (b) 1H-1,2,4-triazol-1-yl, (c ) 2-methyl-1H-imidazol-1-yl, (d) piperidin-1-yl, (e) N, N'-dicyclohexylcarbamimidoyloxy, (f) N, N'-diisopropylcarbamimidoyloxy, (g) N '- (3 - (dimethylamino) propyl) -N-ethylcarbamimidoyloxy, (h) 2,5-dioxopyrrolidin-1-yloxy, or (i) 1,3-dioxoisoindolin-2-yloxy, comprising: i) activation of a compound of formula ( II): ** Formula ** with an activating agent selected, respectively, from (a) carbonyldiimidazole (CDI), (b) 1,1'-carbonyl-di- (1,2,4-triazole) (CDT), (c) 1,1'-carbonyl-bis- (2-methylimidazole), (d) 1,1'-carbonyl-dipiperidine, (e) N, N'-dicyclohexylcarbodiimide (DCC), (f) N, N ' -diisopropylcarbodiimide (DIC), (g) 1-ethyl-3- (3-dimethylaminopropyl) carbodiimide (EDC) and a combination of one of the above with (h) N-hydroxysuccinimide or (i) N-hydroxyphthalimide, in a solvent suitable, and optionally ii) isolate the compound of formula (IV).Un procedimiento para preparar un compuesto de fórmula (IV): **Fórmula** donde L es (a) 1H-imidazol-1-ilo, (b) 1H-1,2,4-triazol-1-ilo, (c) 2-metil-1H-imidazol-1-ilo, (d) piperidin-1-ilo, (e) N,N'-diciclohexilcarbamimidoiloxi, (f) N,N'-diisopropilcarbamimidoiloxi, (g) N'-(3-(dimetilamino)propil)-N-etilcarbamimidoiloxi, (h) 2,5-dioxopirrolidin-1-iloxi, o (i) 1,3-dioxoisoindolin-2-iloxi, que comprende: i) activación de un compuesto de fórmula (II): **Fórmula** con un agente activante seleccionado, respectivamente, de (a) carbonildiimidazol (CDI), (b) 1,1'-carbonil-di-(1,2,4-triazol) (CDT), (c) 1,1'-carbonil-bis-(2-metilimidazol), (d) 1,1'-carbonil-dipiperidina, (e) N,N'-diciclohexilcarbodiimida (DCC), (f) N,N'-diisopropilcarbodiimida (DIC), (g) 1-etil-3-(3-dimetilaminopropil)carbodiimida (EDC) y una combinación de uno de los anteriores con (h) N-hidroxisuccinimida o (i) N-hidroxiftalimida, en un disolvente adecuado, y opcionalmente ii) aislar el compuesto de fórmula (IV).
