Trifluoroacetic acid → cis-3-(1H-indazol-5-ylamino)-5-(2-aminocyclohexylamino)pyrazine-2-carboxamide

HRID 2200484

反応式

[NH:1]1[C:9]2[C:4](=[CH:5][C:6]([NH:10][C:11]3[C:12]([C:18]([NH2:20])=[O:19])=[N:13][CH:14]=[C:15](Cl)[N:16]=3)=[CH:7][CH:8]=2)[CH:3]=[N:2]1.CCN(C(C)C)C(C)C.[C@@H:30]1([NH2:37])[CH2:35][CH2:34][CH2:33][CH2:32][C@@H:31]1[NH2:36].C(O)(C(F)(F)F)=O>CN1C(=O)CCC1.O>[NH:1]1[C:9]2[C:4](=[CH:5][C:6]([NH:10][C:11]3[C:12]([C:18]([NH2:20])=[O:19])=[N:13][CH:14]=[C:15]([NH:36][C@@H:31]4[CH2:32][CH2:33][CH2:34][CH2:35][C@@H:30]4[NH2:37])[N:16]=3)=[CH:7][CH:8]=2)[CH:3]=[N:2]1

参加物

反応条件

温度: 150 °C

実験手順

To 3-(1H-indazol-5-ylamino)-5-chloropyrazine-2-carboxamide (˜100 mg) in ˜3 mL NMP was added 6 equivalents of DIEA and 20 equivalents of racemic cis-1,2-cyclohexanediamine. The mixture was heated at 150° C. in a sealed tube overnight. The reaction mixture was cooled, acidified with TFA, diluted with water and prepped via rpHPLC to give the title compound. MS found for C18H22N8O as (M+H)+367.2.

後処理

temperatureThe reaction mixture was cooled

出典と根拠

ORDレコード: ord-8f706c864dd44eba8f00c85172298f84
出典データセット: uspto-grants-2016_06
DOI: 10.6084/m9.figshare.5104873.v1
特許番号: US09359308B2

反応式

参加物

反応物 4

生成物 1

試薬・触媒・溶媒 2

反応条件

実験手順

後処理

出典と根拠

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