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HRID 2200484作成日:2026年10月25日

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

https://huagongshe.com/reaction/2200484

反応式

関与物質

役割名称HCID仕込み量
反応物Trifluoroacetic acidHCID 6422—
反応物DiisopropylethylamineHCID 81531—
反応物1,2-Diaminocyclohexane, cis-HCID 342917—
反応物3-(1H-indazol-5-ylamino)-5-chloropyrazine-2-carboxamideHCID 86685602—
溶媒WaterHCID 962—
溶媒N-methyl-2-pyrrolidoneHCID 13387—
生成物cis-3-(1H-indazol-5-ylamino)-5-(2-aminocyclohexylamino)pyrazine-2-carboxamideHCID 86685601—

反応条件

温度150 °C

反応手順

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.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09359308B2
出典データセットuspto-grants-2016_06
ORD IDord-8f706c864dd44eba8f00c85172298f84
出典メモuspto-grants-2016_06