Triethylamine → N-(6-Chloro-3,4-dihydrospiro[chromene-2,1'-cyclobutan]-4-yl)-2-(5-methoxy-2-methyl-1H-indol-3-yl)acetamide

HRID 452262

反応式

HRID 452262 の反応式
CC1(C)C[CH:10]([NH2:12])[C:9]2[C:4](=[CH:5][CH:6]=[CH:7]C=2)[O:3]1.[CH3:14][O:15][C:16]1[CH:17]=[C:18]2[C:22](=[CH:23][CH:24]=1)[NH:21][C:20]([CH3:25])=[C:19]2[CH2:26][C:27]([OH:29])=O.CCN=C=NCCCN(C)C.[ClH:41].[CH:42]1[CH:43]=[CH:44][C:45]2N(O)N=N[C:46]=2[CH:47]=1.C(N(CC)CC)C>ClCCl>[Cl:41][C:42]1[CH:47]=[C:46]2[C:45](=[CH:44][CH:43]=1)[O:3][C:4]1([CH2:5][CH2:6][CH2:7]1)[CH2:9][CH:10]2[NH:12][C:27](=[O:29])[CH2:26][C:19]1[C:18]2[C:22](=[CH:23][CH:24]=[C:16]([O:15][CH3:14])[CH:17]=2)[NH:21][C:20]=1[CH3:25]

参加物

7

実験手順

The title compound was prepared from Intermediate 2 (200 mg, 0.896 mmol) and (5-methoxy-2-methyl-1H-indol-3-yl)acetic acid (195 mg, 0.896 mmol) in presence of EDCI.HCl (256 mg, 1.345 mmol), HOBt (205 mg, 1.345 mmol) and triethylamine (374 μl, 3.003 mmol) in dichloromethane (10 ml) as described in Example 1 to give 35 mg of the product as a white solid; IR (KBr) 3383, 2934, 2343, 1648, 1475, 1217, 820 cm−1; 1H NMR (300 MHz, CDCl3) δ 1.50-1.65 (m, 5H), 1.83-1.95 (m, 3H), 2.40 (s, 3H), 3.73 (s, 3H), 3.82 (s, 2H), 5.23 (q, J=9.6 Hz, 1H), 5.76 (d, J=8.7 Hz, 1H), 6.62 (d, J=8.4 Hz, 1H), 6.77 (dd, J=2.4, 6.6 Hz, 1H), 6.82-6.89 (m, 2H), 6.98 (dd, J=2.1, 6.3 Hz, 1H), 7.14 (d, J=8.4 Hz, 1H), 7.84 (s, 1H); ESI-MS (m/z) 423.58 (M−H)−.

出典と根拠

ORDレコード
ord-d5baacfe4c6e4c708efa07ca1ad92164
出典データセット
uspto-grants-2013_07
特許番号
US08487121B2

関連ノート

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