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Last Updated: April 23, 2024

Details for Patent: 7,563,892


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Title:Prodrugs of 2,4 pyrimidinediamine compounds and their uses
Abstract: The present disclosure provides the 2,4-pyrimidinediamine compound shown below, compositions comprising the compound, intermediates and methods for synthesizing the compound, and methods of using the compound in a variety of applications including treatment of autoimmune diseases. ##STR00001##
Inventor(s): Singh; Rajinder (Belmont, CA), Bhamidipati; Somasekhar (Foster City, CA), Stella; Valentino J. (Lawrence, KS), Sun; Thomas (Fremont, CA)
Assignee: Rigel Pharmaceuticals, Inc. (South San Francisco, CA)
Filing Date:Oct 05, 2006
Application Number:11/539,074
Claims:1. A method of making a compound according to formula 3, and salts thereof, comprising: (a) reacting compound 1: ##STR00032## with di-tert-butyl chloromethyl phosphate under conditions to make compound 2: ##STR00033## (b) exposing 2 to an acid to give compound 3; and ##STR00034## (c) exposing 3 to an aqueous base.

2. The method of claim 1, wherein the said conditions in (a) comprise a base.

3. The method of claim 2, wherein the base is cesium carbonate.

4. The method of claim 2, wherein the said conditions in (a) further comprise an organic solvent.

5. The method of claim 4, wherein the organic solvent is dimethylformamide.

6. The method of claim 1, wherein the acid in (b) is acetic acid.

7. The method of claim 1, wherein the aqueous base in (c) is a sodium ion containing base.

8. The method of claim 7, wherein the sodium ion containing base is employed to form a disodium salt of compound 3.

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