N-[4-(2-Amino-4-methyl-phenylsulfanyl)-phenyl]-acetamide → N-{4-[4-Methyl-2-(2-methylsulfanyl-thiazolo[4,5-d]pyrimidin-7-ylamino)-phenylsulfanyl]-phenyl}-acetamide

HRID 607268노트

반응식

HRID 607268 반응식
[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]([CH3:22])[CH:19]=[CH:18][C:17]=1[S:23][C:24]1[CH:29]=[CH:28][C:27]([NH:30][C:31](=[O:33])[CH3:32])=[CH:26][CH:25]=1.NC1C=C(OCC2C=CC=C(Br)C=2)C=CC=1SC1C=CC(O)=CC=1>>[CH3:22][C:20]1[CH:21]=[CH:16][C:17]([S:23][C:24]2[CH:29]=[CH:28][C:27]([NH:30][C:31](=[O:33])[CH3:32])=[CH:26][CH:25]=2)=[C:18]([NH:2][C:1]2[C:3]3[S:7][C:6]([S:8][CH3:9])=[N:5][C:4]=3[N:10]=[CH:11][N:12]=2)[CH:19]=1

참가 물질

4

반응물 3

HCID 43168935N-[4-(2-Amino-4-methyl-phenylsulfanyl)-phenyl]-acetamide2회HCID 668082684-[2-Amino-4-(3-bromo-benzyloxy)-phenylsulfanyl]-phenolHCID 66808347N'-(5-Cyano-2-methylsulfanyl-thiazol-4-yl)-N,N-dimethyl-formamidine

생성물 1

HCID 66808436N-{4-[4-Methyl-2-(2-methylsulfanyl-thiazolo[4,5-d]pyrimidin-7-ylamino)-phenylsulfanyl]-phenyl}-acetamide수율 83%

실험 절차

A solution of the product from Example 167A and the product from Example 7b were reacted according to the procedure from Example 167B substituting the product from Example 7b for the product from Example 15A to provide the crude material which was purified by trituration with methanol to provide the title compound (110 mg, 83%). 1H NMR (300 MHz, DMSO-D6) δ ppm: 2.03 (s, 3H), 2.29 (s, 3H), 2.76 (s, 3H), 6.96 (d, J=8.09 Hz, 1H), 7.14 (d, J=8.09 Hz, 1H), 7.18-7.26 (m, J=8.82 Hz, 3H), 7.54 (d, J=8.46 Hz, 2H), 8.45 (s, 1H), 9.74 (s, 1H), 10.04 (s, 1H); MS (ESI)+ m/z 454 (M+H)+.

후처리

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

출처 및 근거

ORD 기록
ord-cb8a24e8f0d64d2a8312696fd8ac7319
출처 데이터셋
uspto-grants-2011_03
특허 번호
US07915411B2

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