تفاعل #1356980

معادلة التفاعل

diethyl azodicarboxylate toluene

4-hydroxytetrahydropyran

triphenylphosphine

1H-indazol-5-ol

→

5-(tetrahydro-2H-pyran-4-yloxy)-1H-indazole

المردود 47.0%

المذيبات

tetrahydrofuran

ظروف التفاعل

المعالجة

1. 1
   أخرىat 0° C
2. 2
   أخرىthe mixture thus obtained
3. 3
   تركيزthe reaction solution was concentrated under reduced pressure
4. 4
   أخرىthe resulting residue was purified by a silica gel column chromatography (eluent: chloroform/methanol)

الإجراء التجريبي

To a solution of the 1H-indazol-5-ol (150 mg, 1.12 mmol) obtained in Reference Example 4 in tetrahydrofuran (6 ml) were added 4-hydroxytetrahydropyran (0.107 ml, 1.12 mmol), triphenylphosphine (293 mg, 1.12 mmol) and a 40%-diethyl azodicarboxylate-toluene solution (0.517 ml, 1.14 mmol) at 0° C. After 30 minutes, the mixture thus obtained was heated to room temperature. After stirring overnight, the reaction solution was concentrated under reduced pressure, and the resulting residue was purified by a silica gel column chromatography (eluent: chloroform/methanol) to obtain 5-(tetrahydro-2H-pyran-4-yloxy)-1H-indazole (11.4 mg, 47%).

المصدر