تفاعل #1356993

معادلة التفاعل

methylamine ethanolamine

cis-2-[4-(1H-indazol-5-yloxy)cyclohexyl]-1H-isoindole-1,3(2H)-dione

→

cis-4-(1H-indazol-5-yloxy)cyclo-hexanamine

المردود 57.0%

المذيبات

water

ظروف التفاعل

المعالجة

1. 1
   أخرىthe mixture thus obtained
2. 2
   استخلاصextracted with ethyl acetate (20 ml×2)
3. 3
   تجفيفthe organic layer was dried over anhydrous magnesium sulfate
4. 4
   أخرىThe organic layer dried
5. 5
   تركيزwas concentrated under reduced pressure
6. 6
   أخرىthe resulting residue was purified by a silica gel column chromatography (eluent: chloroform/methanol→chloroform/methanol/(1%-aqueous ammonia))

الإجراء التجريبي

A 30%-methylamine-ethanolamine solution (1.0 ml) was added to the cis-2-[4-(1H-indazol-5-yloxy)cyclohexyl]-1H-isoindole-1,3(2H)-dione (100 mg, 0.277 mmol) obtained in Example 380. After 22 hours, the mixture thus obtained was poured into water (20 ml) and extracted with ethyl acetate (20 ml×2), and the organic layer was dried over anhydrous magnesium sulfate. The organic layer dried was concentrated under reduced pressure, and the resulting residue was purified by a silica gel column chromatography (eluent: chloroform/methanol→chloroform/methanol/(1%-aqueous ammonia)) to obtain cis-4-(1H-indazol-5-yloxy)cyclo-hexanamine (36 mg, 57%).

المصدر