2-difluoromethyl-4-hydroxy-2,3-dihydro-benzofuran-6-carboxylic acid (1-methyl-1H-pyrazol-3-yl)-amide → HCID 59560312、化合物

HRID 1177231

反応式

HRID 1177231 の反応式
[N:1]1([C:5]([C:7]2[CH:12]=[CH:11][C:10](F)=[CH:9][CH:8]=2)=[O:6])[CH2:4][CH2:3][CH2:2]1.[CH3:14][N:15]1[CH:19]=[CH:18][C:17]([NH:20][C:21]([C:23]2[CH:34]=[C:33]([OH:35])[C:26]3[CH2:27][CH:28]([CH:30]([F:32])[F:31])[O:29][C:25]=3[CH:24]=2)=[O:22])=[N:16]1>>[CH3:14][N:15]1[CH:19]=[CH:18][C:17]([NH:20][C:21]([C:23]2[CH:34]=[C:33]([O:35][C:10]3[CH:11]=[CH:12][C:7]([C:5]([N:1]4[CH2:4][CH2:3][CH2:2]4)=[O:6])=[CH:8][CH:9]=3)[C:26]3[CH2:27][CH:28]([CH:30]([F:32])[F:31])[O:29][C:25]=3[CH:24]=2)=[O:22])=[N:16]1

参加物

3

反応物 2

HCID 595604162-difluoromethyl-4-hydroxy-2,3-dihydro-benzofuran-6-carboxylic acid (1-methyl-1H-pyrazol-3-yl)-amideHCID 66755817Azetidin-1-yl(4-fluorophenyl)methanone

生成物 1

HCID 59560312HCID 59560312、化合物

実験手順

The title compound was prepared in a similar manner as described for Example 33, from azetidin-1-yl(4-fluorophenyl)methanone (57.4 mg, 0.32 mmol) and 2-difluoromethyl-4-hydroxy-2,3-dihydro-benzofuran-6-carboxylic acid (1-methyl-1H-pyrazol-3-yl)-amide (223a) (99 mg, 0.32 mmol) to give a white solid (12 mg, 8% yield). 1H NMR (400 MHz, CDCl3) δ 8.86 (s, 1 H) 7.55-7.71 (m, 2 H) 7.22-7.31 (m, 1 H) 7.13-7.19 (m, 1 H) 7.06-7.12 (m, 1 H) 6.96-7.03 (m, 2 H) 6.79 (d, J=2.02 Hz, 1 H) 5.75-6.08 (m, 1 H) 4.93-5.19 (m, 1 H) 4.35 (br. s., 2 H) 4.24 (br. s., 2 H) 3.79 (s, 3 H) 3.57-3.63 (m, 1 H) 3.14-3.31 (m, 2 H) 2.30-2.42 (m, 1H.); LCMS for C24H22F2N4O4 m/z 469.00 (M+H)+.

出典と根拠

ORDレコード
ord-7949e5e6f88f4cebb4b252462c542f57
出典データセット
uspto-grants-2010_11
特許番号
US07842713B2

関連ノート

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