5-(5,6-difluoro1H-indol-2-yl)-2-methoxy-phenylamine → (4-{3-[5-(5,6-Difluoro-1h-indol-2-yl)-2-methoxy-phenyl]-thioureido}-benzyl)-phosphonic acid diethyl ester

HRID 25514

反応式

HRID 25514 の反応式
[F:1][C:2]1[CH:3]=[C:4]2[C:8](=[CH:9][C:10]=1[F:11])[NH:7][C:6]([C:12]1[CH:13]=[CH:14][C:15]([O:19][CH3:20])=[C:16]([NH2:18])[CH:17]=1)=[CH:5]2.[N:21]([C:24]1[CH:38]=[CH:37][C:27]([CH2:28][P:29](=[O:36])([O:33][CH2:34][CH3:35])[O:30][CH2:31][CH3:32])=[CH:26][CH:25]=1)=[C:22]=[S:23]>>[CH2:31]([O:30][P:29]([CH2:28][C:27]1[CH:26]=[CH:25][C:24]([NH:21][C:22]([NH:18][C:16]2[CH:17]=[C:12]([C:6]3[NH:7][C:8]4[C:4]([CH:5]=3)=[CH:3][C:2]([F:1])=[C:10]([F:11])[CH:9]=4)[CH:13]=[CH:14][C:15]=2[O:19][CH3:20])=[S:23])=[CH:38][CH:37]=1)(=[O:36])[O:33][CH2:34][CH3:35])[CH3:32]

参加物

3

反応物 2

HCID 99434395-(5,6-difluoro1H-indol-2-yl)-2-methoxy-phenylamine2 回HCID 22568434Diethyl 4-isothiocyanatobenzylphosphonate

生成物 1

HCID 87999803(4-{3-[5-(5,6-Difluoro-1h-indol-2-yl)-2-methoxy-phenyl]-thioureido}-benzyl)-phosphonic acid diethyl ester

実験手順

The product from Example 3, 5-(5,6-difluoro-1H-indol-2-yl)-2-methoxy-phenylamine, (0.137 g, 0.5 mmol) was reacted with the product from Example 23, Step A (0.156 g, 0.54 mmol) according to the procedure for Example 23, Step B to give the product (0.172 g), mp 180-182° C.

出典と根拠

ORDレコード
ord-fdf2a18672704ebf834b4895c6e25952
出典データセット
uspto-grants-2005_02
特許番号
US06858739B2

関連ノート

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