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Serving leading biopharmaceutical companies globally:

Federal Trade Commission
Queensland Health
Fish and Richardson

Generated: February 24, 2018

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Claims for Patent: 4,642,346

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Summary for Patent: 4,642,346
Title: Anhydrous crystalline 9-(1,3-dihydroxy-2-propoxymethyl)guanine
Abstract:Novel anhydrous crystalline 9-(1,3-dihydroxy-2-propoxymethyl)guanine useful as an antiviral agent.
Inventor(s): Chan; Tai W. (Palo Alto, CA), Nguyen; Huong T. (Saratoga, CA)
Assignee: Syntex (U.S.A.) Inc. (Palo Alto, CA)
Application Number:06/747,631
Patent Claims: 1. Anhydrous crystalline 9-(1,3-dihydroxy-2-propoxymethyl)guanine.

2. The anhydrous crystals of claim 1 further characterized by water of hydration of less than 1% w/w.

3. The anhydrous crystals of claim 2 further characterized by m.p. 243.degree. C.-245.degree. C.

4. The anhydrous crystals of claim 3 characterized by the powder X-ray diffraction pattern shown in FIGS. IA, IB or IC.

5. The process for preparing the anhydrous crystals of claim 1 which comprises

(i) adding 9-(1,3-dihydroxy-2-propoxymethyl)guanine to a heated oxygen-containing solvent;

(ii) cooling the mixxture formed in step (i) to room temperature; and

(iii) recovering the crystals formed in step (ii).

6. The process of claim 5 wherein the oxygen-containing solvent is dimethyl acetamide or water.

7. The process of claim 6 wherein the solvent is warmed to 60.degree. to 100.degree. C.

8. The process of claim 7 which further comprises adding methanol or acetone to the warm solution.

9. The process of claim 5 wherein the oxygen-containing solvent is an alcohol of one to four carbon atoms.

10. The process of claim 9 wherein the solvent is warmed to 40.degree. to 80.degree. C.

11. A process for preparing the anhydrous crystals of claim 1 which comprises heating a suitable form of 9-(1,3-dihydroxy-2-propoxymethyl)guanine.

12. The process of claim 11 wherein the suitable form is 9-(1,3-dihydroxy-2-propoxymethyl)guanine hydrate.

13. The process of claim 12 wherein the hydrate is heated to 200.degree.-220.degree. C.

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