Trifluoroacetic acid → methyl 1-(4-fluorobenzyl)-3-(3-(2-methylpyridin-4-yl)-1H-indazole-5-carboxamido)cyclohexanecarboxylate

HRID 530876ノート

反応式

HRID 530876 の反応式
[F:1][C:2]1[CH:56]=[CH:55][C:5]([CH2:6][C:7]2([C:51]([O:53][CH3:54])=[O:52])[CH2:12][CH2:11][CH2:10][CH:9]([NH:13][C:14]([C:16]3[CH:17]=[C:18]4[C:22](=[CH:23][CH:24]=3)[N:21](C(C3C=CC=CC=3)(C3C=CC=CC=3)C3C=CC=CC=3)[N:20]=[C:19]4[C:44]3[CH:49]=[CH:48][N:47]=[C:46]([CH3:50])[CH:45]=3)=[O:15])[CH2:8]2)=[CH:4][CH:3]=1.FC(F)(F)C(O)=O.C([SiH](CC)CC)C>>[F:1][C:2]1[CH:56]=[CH:55][C:5]([CH2:6][C:7]2([C:51]([O:53][CH3:54])=[O:52])[CH2:12][CH2:11][CH2:10][CH:9]([NH:13][C:14]([C:16]3[CH:17]=[C:18]4[C:22](=[CH:23][CH:24]=3)[NH:21][N:20]=[C:19]4[C:44]3[CH:49]=[CH:48][N:47]=[C:46]([CH3:50])[CH:45]=3)=[O:15])[CH2:8]2)=[CH:4][CH:3]=1

参加物

4

反応物 3

HCID 6422Trifluoroacetic acidHCID 12052TriethylsilaneHCID 67985845methyl 1-(4-fluorobenzyl)-3-(3-(2-methylpyridin-4-yl)-1-trityl-1H-indazole-5-carboxamido)cyclohexanecarboxylate

生成物 1

HCID 67985855methyl 1-(4-fluorobenzyl)-3-(3-(2-methylpyridin-4-yl)-1H-indazole-5-carboxamido)cyclohexanecarboxylate

実験手順

In a flask, methyl 1-(4-fluorobenzyl)-3-(3-(2-methylpyridin-4-yl)-1-trityl-1H-indazole-5-carboxamido)cyclohexanecarboxylate (230 mg, 0.31 mmol) was reacted with trifluoroacetic acid (3 mL) for 1 hour. After reaction completion triethylsilane (0.1 mL) was added, and the reaction was stirred for an additional 15 minutes. The reaction was concentrated and rinsed with diethyl ether. The crude product was progressed to the next step without further purification.

後処理

  1. additionwas added
  2. concentrationThe reaction was concentrated
  3. washrinsed with diethyl ether
  4. customThe crude product was progressed to the next step without further purification

出典と根拠

ORDレコード
ord-c8d813e91f5349d69206a1ce63d87b7d
出典データセット
uspto-grants-2016_05
特許番号
US09351965B2

反応ノート

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