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US 2009/0069563 A1Published application
Rosuvastatin intermediates and their preparation
OwnerValerie Niddam-Hildesheim, Anna Balanovinventors
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Abstract
Provided are processes and intermediates for preparation of rosuvastatin.
Claims59
A compound, 19 OH-XYPO, of the following formula:
- wherein X is O, N, or S, and Y is selected from the group consisting of:
- a C1-C4 alkyl, C6 to C12 aryl, and C6 to C12 alkyl aryl group.
A compound, 19-OH-MBSG-XY, of the following formula:
- wherein X is O, N, or S, and Y is selected from the group consisting of:
- a C1-C4 alkyl, C6 to C12 aryl, and C6 to C12 alkyl aryl group, wherein the compound has a purity of at least about 95.5% as measured by GC.
A process for purifying a one or more of rosuvastatin intermediates 19 OH-XYPO of formula:
- or OH-MBSG-XY of formula:
- wherein X is O, N, or S, and Y is selected from the group consisting of:
- a C1-C4 alkyl, C6 to C12 aryl, and C6 to C12 alkyl aryl group,
- comprising applying a force under pressure of less than one atmosphere to increase surface area of a feed containing the intermediate, thereby providing the intermediate in purified form.
1 more element
A process for preparing compound TB21:
- comprising combining OH-MBSG having the following formula:
- DMMP and a base which is capable of making a carbanion on DMMP to obtain a non protected hydroxyl group intermediate 19 OH-TBPO having the following formula:
- and combining the obtained 19 OH-TBPO with FPP-aldehyde and a base.
Dependencies are inferred from the claim text.