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US 6,444,826 B1Granted
Processes and intermediates for preparing substituted chromanol derivatives
AssigneePfizer Inc.
InventorsAnthony Piscopio, Joel M. Hawkins, Stephane Caron, Sarah E. Kelly, Jeffrey W. Raggon, Michael J. Castaldi, Robert W. Dugger, Sally G. Ruggeri
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Abstract
The invention relates to processes for preparing a compound of the formula and the enantiomer of said compound, wherein the benzoic acid moiety is attached at position 6 or 7 of the chroman ring, and R1, R2, and R3 are as defined herein. The invention further relates to intermediates that are useful in the preparation of the compound of formula X above.
Claims1
A compound of the formula
- or the enantiomer of said compound, wherein X is attached at position 4 or 5 of the phenyl moiety;
- R1 is —(CH2)qCHR5R6 wherein q is 0 to 4;
- each R2 is independently selected from the group consisting of H, fluoro, chloro, C1-C6 alkyl, C1-C6 alkoxy, phenylsulfinyl, phenylsulfonyl, and —S(O)n, (C1-C6 alkyl) wherein n is 0 to 2, and wherein said alkyl group, the alkyl moiety of said alkoxy and —S(O)n(C1-C6 alkyl) groups, and the phenyl moiety of said phenylsulfinyl and phenylsulfonyl groups are optionally substituted by 1 to 3 fluoro groups;
- R5 is H, C1-C6 alkyl, or phenyl substituted by R2;
- R6 is H, C1-C6 alkyl, C3-C8 cycloalkyl, C6-C10 aryl, or 5-10 membered heteroaryl, wherein said aryl and heteroaryl groups are optionally substituted by 1 or 2 substituents independently-selected from phenyl, R2, and phenyl substituted by 1 or 2 R2;
- X is halo;
- Y is halo or nitro;
- and,
- Xc is a chiral auxiliary.
6 more elements
Dependencies are inferred from the claim text.