4-[2-Amino-4-(3-bromo-benzyloxy)-phenylsulfanyl]-phenol → 4-[4-(4-Bromo-benzyloxy)-2-(2-methylsulfanyl-thiazolo[4,5-d]pyrimidin-7-ylamino)-phenylsulfanyl]-phenol

HRID 607267ノート

反応式

HRID 607267 の反応式
[C:1]([C:3]1[S:7][C:6]([S:8][CH3:9])=[N:5][C:4]=1[N:10]=[CH:11][N:12](C)C)#[N:2].N[C:16]1[CH:21]=[C:20]([O:22][CH2:23][C:24]2[CH:29]=[CH:28][C:27]([Br:30])=[CH:26][CH:25]=2)[CH:19]=[CH:18][C:17]=1[S:31][C:32]1[CH:37]=[CH:36][C:35]([OH:38])=[CH:34][CH:33]=1.NC1C=C(OCC2C=CC=C(Br)C=2)C=CC=1SC1C=CC(O)=CC=1>>[Br:30][C:27]1[CH:28]=[CH:29][C:24]([CH2:23][O:22][C:20]2[CH:19]=[CH:18][C:17]([S:31][C:32]3[CH:37]=[CH:36][C:35]([OH:38])=[CH:34][CH:33]=3)=[C:16]([NH:2][C:1]3[C:3]4[S:7][C:6]([S:8][CH3:9])=[N:5][C:4]=4[N:10]=[CH:11][N:12]=3)[CH:21]=2)=[CH:25][CH:26]=1

参加物

4

反応物 3

HCID 668082684-[2-Amino-4-(3-bromo-benzyloxy)-phenylsulfanyl]-phenolHCID 668082894-[2-Amino-4-(4-bromo-benzyloxy)-phenylsulfanyl]-phenol2 回HCID 66808347N'-(5-Cyano-2-methylsulfanyl-thiazol-4-yl)-N,N-dimethyl-formamidine

生成物 1

HCID 668084654-[4-(4-Bromo-benzyloxy)-2-(2-methylsulfanyl-thiazolo[4,5-d]pyrimidin-7-ylamino)-phenylsulfanyl]-phenol収率 27%

実験手順

A solution of the product from Example 167A and the product from Example 16A were reacted according to the procedure from Example 167B substituting the product from Example 16A for the product from Example 15A to provide the crude material which was purified by trituration with methanol to provide the title compound as a white solid (46 mg, 27%). 1H NMR (300 MHz, DMSO-D6) δ ppm: 2.76 (s, 3H), 5.09 (s, 2H), 6.70 (d, J=8.46 Hz, 2H), 6.91-7.24 (m, 5H), 7.38 (d, J=8.09 Hz, 2H), 7.56 (d, J=8.09 Hz, 2H), 8.46 (s, 1H), 9.71 (s, 2H); MS (ESI)+ m/z 583/585 (M+H)+.

後処理

  1. customto provide the crude material which
  2. customwas purified by trituration with methanol

出典と根拠

ORDレコード
ord-8ee15170f6fb4b46a998c0ecd9f56ee1
出典データセット
uspto-grants-2011_03
特許番号
US07915411B2

反応ノート

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