(1-methyl-1H-pyrazol-4-yl)methanamine → HCID 57919917, 화합물

HRID 554989

반응식

HRID 554989 반응식
FC1C=C(CN)C=NC=1.[CH3:10][N:11]1[CH:15]=[C:14]([CH2:16][NH2:17])[CH:13]=[N:12]1.[CH3:18][C:19]1[N:20]=[C:21]([N:27]2[CH2:31][CH2:30][N:29]([CH2:32][CH2:33][CH2:34][C:35]([F:38])([F:37])[F:36])[C:28]2=[O:39])[S:22][C:23]=1[C:24](O)=[O:25]>>[CH3:18][C:19]1[N:20]=[C:21]([N:27]2[CH2:31][CH2:30][N:29]([CH2:32][CH2:33][CH2:34][C:35]([F:36])([F:37])[F:38])[C:28]2=[O:39])[S:22][C:23]=1[C:24]([NH:17][CH2:16][C:14]1[CH:13]=[N:12][N:11]([CH3:10])[CH:15]=1)=[O:25]

참가 물질

4

반응물 3

HCID 671225(1-methyl-1H-pyrazol-4-yl)methanamineHCID 45116207(5-Fluoropyridin-3-yl)methanamineHCID 579198994-Methyl-2-(2-oxo-3-(4,4,4-trifluorobutyl)imidazolidin-1-yl)thiazole-5-carboxylic acid

생성물 1

HCID 57919917HCID 57919917, 화합물수율 49%

실험 절차

Following the procedure as describe in Example 12, making variations as required to replace (5-fluoropyridin-3-yl)methanamine with (1-methyl-1H-pyrazol-4-yl)methanamine to react with 4-methyl-2-(2-oxo-3-(4,4,4-trifluorobutyl)imidazolidin-1-yl)thiazole-5-carboxylic acid in place of 2-(3-(cyclopropylmethyl)-2-oxoimidazolidin-1-yl)-4-methylthiazole-5-carboxylic acid, the title compound was obtained as a colorless solid in 49% yield: 1H NMR (300 MHz, CDCl3) δ 7.44 (s, 1H), 7.37 (s, 1H), 5.79-5.76 (m, 1H), 4.40 (d, J=5.3 Hz, 2H), 4.15-4.09 (m, 2H), 3.87 (s, 3H), 3.62-3.57 (m, 2H), 3.42-3.37 (m, 2H), 2.60 (s, 3H), 2.19-2.11 (m, 2H), 1.88-1.83 (m, 2H); 13C NMR (75 MHz, CDCl3) δ 162.2, 157.1, 155.6, 152.8, 138.7, 129.4, 118.2, 117.4, 42.9, 42.3, 42.0, 38.9, 34.4, 31.4, 30.9, 20.2, 17.2; MS (ES+) m/z 430.9 (M+1).

출처 및 근거

ORD 기록
ord-79d19526017f43c2a1e5e7af4b62acc0
출처 데이터셋
uspto-grants-2011_11
특허 번호
US08049016B2

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