Technology Process of 3-{2-[4-(4-fluoro-2-hydroxybenzoyl)piperidin-1-yl]ethyl}-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one
There total 6 articles about 3-{2-[4-(4-fluoro-2-hydroxybenzoyl)piperidin-1-yl]ethyl}-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one which
guide to synthetic route it.
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synthetic route:
- Guidance literature:
-
paliperidone;
With
hydrogen; sodium hydroxide;
palladium 10% on activated carbon;
In
methanol; water;
at 25 - 35 ℃;
for 2h;
Inert atmosphere;
With
hydrogenchloride;
In
methanol; water;
pH=2.5 - 3;
With
ammonia;
In
water;
at 25 - 30 ℃;
for 0.5h;
pH=5 - 5.5;
- Guidance literature:
-
Multi-step reaction with 4 steps
1.1: trichlorophosphate / 1 h / 30 - 35 °C
1.2: 24 h / 35 - 40 °C
2.1: hydrogen / palladium 10% on activated carbon / methanol / 2 h / 50 - 55 °C / Inert atmosphere
2.2: Inert atmosphere
2.3: 2 h / 5 - 85 °C
3.1: sodium carbonate / methanol / 70 - 75 °C / Inert atmosphere; Pressure vessel
4.1: hydrogen; sodium hydroxide / palladium 10% on activated carbon / water; methanol / 2 h / 25 - 35 °C / Inert atmosphere
4.2: pH 2.5 - 3
4.3: 0.5 h / 25 - 30 °C / pH 5 - 5.5
With
hydrogen; sodium carbonate; sodium hydroxide; trichlorophosphate;
palladium 10% on activated carbon;
In
methanol; water;
- Guidance literature:
-
Multi-step reaction with 4 steps
1.1: trichlorophosphate / 1 h / 30 - 35 °C
1.2: 24 h / 35 - 40 °C
2.1: hydrogen / palladium 10% on activated carbon / methanol / 2 h / 50 - 55 °C / Inert atmosphere
2.2: Inert atmosphere
2.3: 2 h / 5 - 85 °C
3.1: sodium carbonate / methanol / 70 - 75 °C / Inert atmosphere; Pressure vessel
4.1: hydrogen; sodium hydroxide / palladium 10% on activated carbon / water; methanol / 2 h / 25 - 35 °C / Inert atmosphere
4.2: pH 2.5 - 3
4.3: 0.5 h / 25 - 30 °C / pH 5 - 5.5
With
hydrogen; sodium carbonate; sodium hydroxide; trichlorophosphate;
palladium 10% on activated carbon;
In
methanol; water;
