Welcome to chemicalbook!
Chinese English Japanese Germany Korea
400-158-6606
Try our best to find the right business for you.
Do not miss inquiry messages Please log in to view all inquiry messages.

Welcome back!

4H-Pyrido[1,2-a]pyriMidin-4-one,2-hydroxy-9-Methyl- synthesis

2synthesis methods
-

Yield: 96.5%

Reaction Conditions:

at 150; for 24 h;

Steps:

1.1
Example 1. W-{2-[(2f?)-Butan-2-ylamino]-9-methyl-4-oxo-4H-pyrido[1 ,2- a]pyrimidin-3-yl}-3,3-dimethylbutanamideStep 1. 2-Hydroxy-9-methyl-4H-pyrido[1 ,2-a]pyrimidin-4-oneA mixture of 2-amino-3-picoline (10.8 g, 100 mmol) and diethyl malonate (76.3 ml_, 500 mmol) was stirred at 150 °C for 24 h. The mixture was cooled to RT, diluted with ethyl acetate (150 ml_), and filtered. The solid was washed with ethyl acetate (100 ml_) to give the titled compound (17.0 g, 96.5%) as a white solid.1H NMR (DMSO-ofe) δ (ppm) 11.43 (br s, 1 H), 8.76 (d, J = 7.0 Hz, 1 H), 7.79 (d, J = 6.6 Hz, 1 H), 7.15-7.10 (m, 1 H), 5.36 (br, 1 H), 2.40 (s, 3H)MS (ES+) 177

References:

PFIZER INC.;SAKURADA, Isao;ZHANG, Lei WO2012/38850, 2012, A1 Location in patent:Page/Page column 29