(6-Methoxypyridin-3-yl)boronic acid → 1-(1-methylethyl)-N-[(6-methyl-2-oxo-4-propyl-1,2-dihydro-3-pyridinyl)methyl]-6-[6-(methyloxy)-3-pyridinyl]-1H-indazole-4-carboxamide

HRID 85435

反応式

HRID 85435 の反応式
Br[C:2]1[CH:3]=[C:4]([C:14]([NH:16][CH2:17][C:18]2[C:19](=[O:28])[NH:20][C:21]([CH3:27])=[CH:22][C:23]=2[CH2:24][CH2:25][CH3:26])=[O:15])[C:5]2[CH:6]=[N:7][N:8]([CH:11]([CH3:13])[CH3:12])[C:9]=2[CH:10]=1.[CH3:29][O:30][C:31]1[N:36]=[CH:35][C:34](B(O)O)=[CH:33][CH:32]=1>>[CH3:12][CH:11]([N:8]1[C:9]2[CH:10]=[C:2]([C:34]3[CH:35]=[N:36][C:31]([O:30][CH3:29])=[CH:32][CH:33]=3)[CH:3]=[C:4]([C:14]([NH:16][CH2:17][C:18]3[C:19](=[O:28])[NH:20][C:21]([CH3:27])=[CH:22][C:23]=3[CH2:24][CH2:25][CH3:26])=[O:15])[C:5]=2[CH:6]=[N:7]1)[CH3:13]

参加物

3

反応物 2

HCID 2734368(6-Methoxypyridin-3-yl)boronic acidHCID 674653266-bromo-1-(1-methylethyl)-N-[(6-methyl-2-oxo-4-propyl-1,2-dihydro-3-pyridinyl)methyl]-1H-indazole-4-carboxamide

生成物 1

HCID 545967631-(1-methylethyl)-N-[(6-methyl-2-oxo-4-propyl-1,2-dihydro-3-pyridinyl)methyl]-6-[6-(methyloxy)-3-pyridinyl]-1H-indazole-4-carboxamide

実験手順

The title compound was prepared in the same manner as described for example 75 from 6-bromo-1-(1-methylethyl)-N-[(6-methyl-2-oxo-4-propyl-1,2-dihydro-3-pyridinyl)methyl]-1H-indazole-4-carboxamide (100 mg, 0.225 mmol) and [6-(methyloxy)-3-pyridinyl]boronic acid (52 mg, 0.337 mmol). The final product was collected as a white solid (72 mg, 67%). 1H NMR (400 MHz, DMSO-d6) δ ppm 11.55 (br. s., 1H) 8.68 (br. s., 1H) 8.62 (br. s., 1H) 8.39 (s, 1H) 8.21 (br. s., 1H) 8.14 (s, 1H) 7.86 (s, 1H) 6.97 (d, J=8.59 Hz, 1H) 5.92 (s, 1H) 5.09-5.21 (m, 1H) 4.37-4.48 (m, 2H) 3.92 (s, 3H) 2.54 (br. s., 2H) 2.14 (s, 3H) 1.55 (m, 2H) 1.51 (br. s., 3H) 1.50 (br. s., 3H) 0.88 (t, J=7.20 Hz, 3H). LC-MS (ES) m/z=474.0

後処理

  1. customThe final product was collected as a white solid (72 mg, 67%)

出典と根拠

ORDレコード
ord-bb4768a97c2947f99f771ba9d6b30982
出典データセット
uspto-grants-2014_09
特許番号
US08846935B2

関連ノート

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