摘要：

Procedure for the preparation of 1- [6- (morpholin-4-yl) pyrimidin-4-yl] -4- (1 H-1,2,3-triazol-1-yl) -1 H -pyrazol-5-ol ( I - enol form) or 2- [6- (morpholin-4-yl) pyrimidin-4-yl] -4- (1H-1,2,3-triazol-1-yl) -1,2-dihydro- 3H-pyrazole-3-one (I-keto form), characterized in that a) in the first stage 1,2,3-triazole (III) is reacted with methyl bromoacetate (IV-Me-Br) or bromoacetate of ethyl (IV-Et-Br) in the presence of ethyldiisopropylamine as a base in a solvent in a temperature range of 20 to 80 ° C to give the compounds methyl acetate-1H-1,2,3-triazol-1-yl (V -Me) and methyl-2H-1,2,3-triazol-1-yl acetate (VI-Me) or the ethyl-1H-1,2,3-triazol-1-yl acetate (VEt) compounds and ethyl-2H-1,2,3-triazol-1-yl acetate (VI-Et), b) in the second stage the methyl acetate-1H-1,2,3-triazol-1-yl compounds ( V-Me) and methyl-2H-1,2,3-triazol-1-yl acetate (VI-Me) or the compounds ethyl acetate-1H-1,2,3-triazol-1-yl (V -Et) and ethyl acetate-2H-1,2,3-triazol-1-i lo (VI-Et), which are in a ratio of at least 6: 1 relative to each other, are reacted with dimethylformamide dimethyl acetal (XIX-Me) or dimethylformamide diethyl acetal (XIX-Et) in a solvent inert and then crystallized by cooling the solution or by distilling off the solvent and adding a second solvent to give the methyl- (2E / Z) -3- (dimethylamino) -2- (1H-1) acrylate, 2,3-triazol-1-yl) (VII-Me) or ethyl acrylate- (2E / Z) -3- (dimethylamino) -2- (1H-1,2,3-triazol-1-yl) (VII-Et) and c) in the third stage, methyl acrylate (2E / Z) -3- (dimethylamino) -2- (1H-1,2,3-triazol-1-yl) (VIIMe) is reacted or ethyl- (2E / Z) -3- (dimethylamino) -2- (1H-1,2,3-triazol-1-yl) (VII-Et) acrylate with 4- (6-hydrazinopyrimidin-4- il) morpholine (XI) in the presence of trifluoroacetic acid in an inert solvent and then the compound of formula (I) is isolated.

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