ZARAGOZA DOERWALD, Florencio,KULESZA, Anna,ELZNER, Stephan,BUJOK, Robert,WROBEL, Zbigniew,WOJCIECHOWSKI, Krzysztof
申请号：
ES12787007
公开号：
ES2565066T3
申请日:
2012.11.15
申请国别(地区):
ES
年份:
2016
代理人:
摘要：
Method of preparing the compound of formula (XX)； ** Formula ** the method comprises four stages, the four stages are a stage (Q1), a stage (Q2), a stage (N) and a stage (M1)； the compound of formula (XX) is prepared in step (M1)； step (M1) comprises a reaction (M1-reac)； the reaction (M1-reac) is a reaction between a compound of formula (XXI), ** Formula ** a reagent (M-rea) and a reagent (M-A) in a solvent (M-disv)； The reagent (M-react) is selected from the group consisting of p-toluenesulfonylmethyl isocyanide, trifluoromethanesulfonylmethyl isocyanide, methanesulfonylmethyl isocyanide, benzenesulfonylmethyl isocyanide, 4-acetamidobenzenesulfonylmethyl isocyanide and mixtures； Reagent (M-A) is selected from the group consisting of ammonia, sulfamic acid, p-toluenesulfonamide, benzenesulfonamide, 4-acetamidobenzenesulfonamide, tritylamine, formamide, urea, urotropin, ethyl carbamate, acetamide and mixtures thereof； The solvent (M-disv) is selected from the group consisting of N, N-dimethylformamide, C1-6 alkanol, formamide, 1,2-dimethoxyethane, NMP, toluene, acetonitrile, propionitrile, ethyl carbamate, N, N- dimethylacetamide, water, acetamide and mixtures thereof； the compound of formula (XXI) is prepared in step (N)； step (N) comprises a reaction (N-reac)； the reaction (N-reac) is a reaction of a compound of formula (XXII) with a catalyst (N-cat)； R1 is Br, Cl, or I； the reagent (Q1-react) is selected from the group consisting of lithium, magnesium, aluminum, zinc, calcium, propylmagnesium chloride, propylmagnesium bromide, butyllithium and mixtures thereof； step (Q2) comprises a reaction (Q2-reac)； the reaction (Q2-reac) is a reaction of the reaction product (Q1-reac) with chloroacetone； the compound of formula (XXII) is prepared by reaction (Q2-reac).Método de preparación del compuesto de fórmula (XX)；**Fórmula** el método comprende cuatro etapas, las cuatro etapas son una etapa (Q1), una etapa (Q2), una etapa (N) y una etapa (M1)； el compuesto de fórmula (X
