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US 8,476,432 B2Granted
Process for the preparation of HMG-COA reductase inhibitors and intermediates thereof
AssigneeYuhan Corporation
InventorsHyun Ju, Sang-Sun Joung, Hyun-Jik Yi, Ja-Heouk Khoo, Jong-Chul Lim, Jae-Gyu Kim
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Abstract
The present invention provides an improved process for preparing HMG-CoA reductase inhibitors such as rosuvastatin calcium, fluvastatin sodium, and pitavastatin calcium under a mild condition, using a novel amide-bond-containing compound having R2—N—O—R1 moiety as a key intermediate. And also, the present invention provides the novel compound, an intermediate useful for the preparation thereof, and a process for the preparation thereof.
Claims19
A process for preparing a compound of Formula 1, comprising converting a compound of Formula 4 to a compound of Formula 1:
- wherein,
- M is an alkali metal or an alkaline earth metal,
- R1 and R2 are independently C1˜C5 alkyl or aryl,
- P1 and P2 are independently an alcohol-protecting group;
- or P1 and P2 are cyclized each other to form a 1,3-diol protecting group selected from the group consisting of:
- wherein R9 and R10 are independently C1˜C10 alkyl or R9 and R10 are cyclized each other to form a pentane ring, a hexane ring, or a heptane ring;
- Z is oxygen or sulfur;
- and Ph is phenyl, and
- Het is
6 more elements
Dependencies are inferred from the claim text.