(S)-2-amino-3-(benzyloxy)-N-(4-(4-fluorophenoxy)phenyl)propanamide → (S)-2-(2-(2H-1,2,3-triazol-2-yl)acetamido)-3-(benzyloxy)-N-(4-(4-fluorophenoxy)phenyl)propanamide

HRID 1630090

反応式

HRID 1630090 の反応式
[NH2:1][C@@H:2]([CH2:20][O:21][CH2:22][C:23]1[CH:28]=[CH:27][CH:26]=[CH:25][CH:24]=1)[C:3]([NH:5][C:6]1[CH:11]=[CH:10][C:9]([O:12][C:13]2[CH:18]=[CH:17][C:16]([F:19])=[CH:15][CH:14]=2)=[CH:8][CH:7]=1)=[O:4].Cl.[N:30]1[N:31]([CH2:35][C:36](O)=[O:37])[N:32]=[CH:33][CH:34]=1>>[N:30]1[N:31]([CH2:35][C:36]([NH:1][C@@H:2]([CH2:20][O:21][CH2:22][C:23]2[CH:24]=[CH:25][CH:26]=[CH:27][CH:28]=2)[C:3]([NH:5][C:6]2[CH:7]=[CH:8][C:9]([O:12][C:13]3[CH:18]=[CH:17][C:16]([F:19])=[CH:15][CH:14]=3)=[CH:10][CH:11]=2)=[O:4])=[O:37])[N:32]=[CH:33][CH:34]=1

参加物

3

反応物 2

HCID 67009137(S)-2-amino-3-(benzyloxy)-N-(4-(4-fluorophenoxy)phenyl)propanamideHCID 670094972-(2H-1,2,3-triazol-2-yl)acetic acid hydrochloride

生成物 1

HCID 67009457(S)-2-(2-(2H-1,2,3-triazol-2-yl)acetamido)-3-(benzyloxy)-N-(4-(4-fluorophenoxy)phenyl)propanamide

実験手順

Proceeding as in Example 1, but substituting (S)-2-amino-3-(benzyloxy)-N-(4-(4-fluorophenoxy)phenyl)propanamide and 2-(2H-1,2,3-triazol-2-yl)acetic acid hydrochloride, gave Compound 138, (S)-2-(2-(2H-1,2,3-triazol-2-yl)acetamido)-3-(benzyloxy)-N-(4-(4-fluorophenoxy)phenyl)propanamide. 1H-NMR (400 MHz, CDCl3): σ 8.33 (s, 1H), 7.75 (s, 1H), 7.52 (s, 1H), 7.38-7.21 (m, 7H), 7.04-7.00 (m, 2H), 6.96-6.89 (m, 4H), 5.29-5.20 (m, 2H), 4.71-4.61 (m, 3H), 4.53 (d, 1H), 4.03 (dd, 1H), 3.53 (t, 1H). MS (EI) for C26H24FN5O4. found 489.9 (MH+).

出典と根拠

ORDレコード
ord-62d167185fc743a7b2f3c4b794ced65c
出典データセット
uspto-grants-2014_07
特許番号
US08791102B2

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