반응 #73348

반응 방정식

2-methyl-1H-indol-5-ol

4-oxo-4,5,6,8-tetrahydro-3H-pyrido[3,4-d]pyrimidine-7-carboxylic acid tert-butyl ester

PyBOP

DBU

→

title compound

4-(2-Methyl-1H-indol-5-yloxy)-5,8-dihydro-6H-pyrido[3,4-d]pyrimidine-7-carboxylic acid tert-butyl ester

반응 조건

후처리

1. 1
   농축At that point the reaction is concentrated under reduced pressure
2. 2
   workup.DISSOLUTIONthe residue is dissolved in EtOAc
3. 3
   세척washed by water and brine
4. 4
   건조The organic layer is dried over sodium sulfate
5. 5
   농축concentrated under reduced pressure
6. 6
   기타The residue is purified by FCC (EtOAc/heptane from 0% to 40%)

실험 절차

To a stirring solution of 4-oxo-4,5,6,8-tetrahydro-3H-pyrido[3,4-d]pyrimidine-7-carboxylic acid tert-butyl ester, Example 31-A, (300 mg, 1.2 mmol) in I (5 mL) is added PyBOP (800 mg, 1.55 mmol) and DBU (0.2 mL, 1.43 mmol). After 20 min 2-methyl-1H-indol-5-ol (211 mg, 1.43 mmol) is added. The mixture is then stirred at room temperature for 16 h. At that point the reaction is concentrated under reduced pressure and the residue is dissolved in EtOAc and washed by water and brine. The organic layer is dried over sodium sulfate, concentrated under reduced pressure. The residue is purified by FCC (EtOAc/heptane from 0% to 40%) to give the title compound. MS (ESI) m/z 381.0 (M+1).

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