Réaction #8812

Équation de réaction

7-Benzyl-4-morpholin-4-yl-5,6,7,8-tetrahydro-pyrido[3,4-d]pyrimidine

7-benzyl-4-morpholin-4-yl-5,6,7,8-tetrahydro-pyrido[3,4-d]pyrimidine

ammonium formate

→

4-morpholin-4-yl-5,6,7,8-tetrahydro-pyrido[3,4-d]pyrimidine

Rendement 69.3%

Solvants

methanol

Conditions de réaction

Traitement

1. 1
   Températurethe mixture was heated
2. 2
   Températureto reflux for 12 h
3. 3
   AutreThe catalyst was removed by filtration
4. 4
   Lavagewashed with MeOH
5. 5
   Concentrationthe filtrate was concentrated
6. 6
   LavageFlash column chromatography eluting with 5% MeOH/CH2Cl2 containing 0.5% of NH4OH

Mode opératoire

7-Benzyl-4-morpholin-4-yl-5,6,7,8-tetrahydro-pyrido[3,4-d]pyrimidine 5a (0.55 g, 1.77 mmol) was dissolved in methanol (35 mL) under nitrogen. 10% Pd/C (0.55 g) was added under nitrogen followed by ammonium formate (1.12 g, 17.72 mmol) and the mixture was heated to reflux for 12 h. The catalyst was removed by filtration, washed with MeOH and the filtrate was concentrated. Flash column chromatography eluting with 5% MeOH/CH2Cl2 containing 0.5% of NH4OH gave 0.27 g of 4-morpholin-4-yl-5,6,7,8-tetrahydro-pyrido[3,4-d]pyrimidine 6a as a pale yellow dense liquid.

Source