Oxolan-3-amine → Rac-5-[3-(5-fluoro-pyridin-2-yl)-5-methyl-isoxazol-4-ylmethoxy]-2-methyl-2H-pyrazole-3-car-boxylic acid (tetrahydro-furan-3-yl)-amide

반응식

CO[C:3]([C:5]1[N:6]([CH3:25])[N:7]=[C:8]([O:10][CH2:11][C:12]2[C:13]([C:18]3[CH:23]=[CH:22][C:21]([F:24])=[CH:20][N:19]=3)=[N:14][O:15][C:16]=2[CH3:17])[CH:9]=1)=[O:4].COC(C1NN=C([O:35][CH2:36][C:37]2[C:38]([C:43]3C=CC=CC=3)=[N:39]OC=2C)C=1)=O.NC1CCOC1>>[O:35]1[CH2:36][CH2:37][CH:38]([NH:39][C:3]([C:5]2[N:6]([CH3:25])[N:7]=[C:8]([O:10][CH2:11][C:12]3[C:13]([C:18]4[CH:23]=[CH:22][C:21]([F:24])=[CH:20][N:19]=4)=[N:14][O:15][C:16]=3[CH3:17])[CH:9]=2)=[O:4])[CH2:43]1

참가 물질

반응물 3

HCID 3365553Oxolan-3-amine

HCID 666436965-[3-(5-Fluoro-pyridin-2-yl)-5-methyl-isoxazol-4-ylmethoxy]-2-methyl-2H-pyrazole-3-carboxylic acid methyl ester

HCID 66643884HCID 66643884, 화합물

생성물 1

HCID 59568407Rac-5-[3-(5-fluoro-pyridin-2-yl)-5-methyl-isoxazol-4-ylmethoxy]-2-methyl-2H-pyrazole-3-car-boxylic acid (tetrahydro-furan-3-yl)-amide수율 59%

실험 절차

As described for example 1b, 5-[3-(5-fluoro-pyridin-2-yl)-5-methyl-isoxazol-4-ylmethoxy]-2-methyl-2H-pyrazole-3-carboxylic acid methyl ester (140 mg, 0.40 mmol), instead of 5-(5-methyl-3-phenyl-isoxazol-4-ylmethoxy)-2H-pyrazole-3-carboxylic acid methyl ester, was converted, using rac-3-aminotetrahydrofuran instead of morpholine, to the title compound (96 mg, 59%) which was obtained as a white solid. MS: m/e=402.3 [M+H]+.