![](/CAS/GIF/17326-09-9.gif)
4H-Pyrido[1,2-a]pyriMidin-4-one,2-hydroxy-9-Methyl- synthesis
- Product Name:4H-Pyrido[1,2-a]pyriMidin-4-one,2-hydroxy-9-Methyl-
- CAS Number:17326-09-9
- Molecular formula:C9H8N2O2
- Molecular Weight:176.17
![2-Amino-3-picoline](/CAS/GIF/1603-40-3.gif)
1603-40-3
480 suppliers
$6.00/25g
![Diethyl malonate](/CAS/GIF/105-53-3.gif)
105-53-3
735 suppliers
$5.00/25g
![4H-Pyrido[1,2-a]pyriMidin-4-one,2-hydroxy-9-Methyl-](/CAS/GIF/17326-09-9.gif)
17326-09-9
28 suppliers
$27.00/250mg
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
![2-Amino-3-picoline](/CAS/GIF/1603-40-3.gif)
1603-40-3
480 suppliers
$6.00/25g
![MALONIC ACID BIS(2,4,6-TRICHLOROPHENYL) ESTER](/CAS/GIF/15781-70-1.gif)
15781-70-1
113 suppliers
$5.00/100mg
![4H-Pyrido[1,2-a]pyriMidin-4-one,2-hydroxy-9-Methyl-](/CAS/GIF/17326-09-9.gif)
17326-09-9
28 suppliers
$27.00/250mg