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US 8,299,242 B2Granted
Synthesis of 2,4-pyrimidinediamines
AssigneeRigel Pharmaceuticals, Inc.
InventorsUlfried Felfer, Karl-Heinz Giselbrecht, Michael Wolberg
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Abstract
Disclosed herein are methods for synthesizing 2,4-pyrimidinediamines as well as intermediates used therein.
Claims8
A process for preparing a compound of formula I:
- comprising:
- a) contacting an acid solvate of a compound of formula II:
- with an amide under conditions suitable for forming an amide solvate of the compound of formula II;
- and
- b) contacting the amide solvate with an aqueous base comprising sodium ions under conditions suitable for forming the compound of formula I
- wherein the carboxylic acid is R1COOH wherein R1 is —H or a C1-C4 alkyl optionally substituted with up to three halo;
- and
- the amide is R30CON(R2)2 where each R2 is independently —H or C1-C4 alkyl or both R2 together with the nitrogen to which they are attached form a 4 to 6 membered aliphatic ring, and R30 is —H or C1-C4 alkyl;
- or R30 and one of the R2 together with the carbon and nitrogen to which they are attached, respectively, combine to form a 4 to 6-membered aliphatic ring and the other R2 is independently —H or C1-C4 alkyl.
6 more elements
Dependencies are inferred from the claim text.