Preparation method for aliskiren
2011
The invention discloses a preparation method for aliskiren. The preparation method comprises the following steps of: preparing a compound (I) from (3S, 5S, 1'S, 3'S)-5-(1'-azido-3'-hydroxymethyl-4'-methyl-amyl)-3-isopropyl-dihydrofuran-2-ketone through catalytic oxidation; performing addition with 4-methoxyl-3-(3-methoxyl propoxy)-bromobenzene under the action of a metal reagent to obtain a compound (II); then performing catalytic hydrogenation and amino group protection to obtain a lactone compound (III), serving an important intermediate of the aliskiren; and finally condensing with 3-amino-2,2-methacrylamide and removing an amino protecting group to obtain the aliskiren. Compared with the prior art, the preparation method has the beneficial effects of cheap and readily available raw materials, short reaction route, easiness and convenience in operation, no special requirement on equipment, high yield, low cost and small environmental protection pressure, is suitable for commercial production and has a higher industrial application value.
Keywords:
- Correction
- Source
- Cite
- Save
- Machine Reading By IdeaReader
0
References
0
Citations
NaN
KQI