반응 #171976

반응 방정식

tert-butyl (1S,2R)-2-(4-cyano-3-(1-methyl-1H-indol-4-ylamino)phenylamino)cyclohexylcarbamate

K2CO3

H2O2

Water

→

titled compound

수율 13.9%

4-((1R,2S)-2-aminocyclohexylamino)-2-(1-methyl-1H-indol-4-ylamino)benzamide

수율 13.9%

용매

EtOAc

DMSO

반응 조건

후처리

1. 1
   기타The organic phase was separated
2. 2
   건조dried over Na2SO4
3. 3
   농축concentrated in vacuo
4. 4
   workup.DISSOLUTIONThe residue was dissolved in TFA (2 mL)
5. 5
   workup.WAITAfter 10 min of standing
6. 6
   기타TFA was removed in vacuo
7. 7
   기타The residue was purified by HPLC

실험 절차

To a solution of tert-butyl (1S,2R)-2-(4-cyano-3-(1-methyl-1H-indol-4-ylamino)phenylamino)cyclohexylcarbamate (90 mg, 0.19 mmol) in DMSO (2 mL). K2CO3 (130 mg, 0.94 mmol) and H2O2 (50% aq., 0.500 mL) were added. The mixture was stirred at 100 C for 10 min. Water and EtOAc were added. The organic phase was separated, dried over Na2SO4, concentrated in vacuo. The residue was dissolved in TFA (2 mL). After 10 min of standing, TFA was removed in vacuo. The residue was purified by HPLC to give the titled compound (10 mg). MS 378.3 (M+H); UV 224.7, 291.5 nm

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