Monohydrate of (1-{9-[4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminopurin-2-yl}pyrazol-4-yl)-N-methylcarboxamide
View Patent ↗Disclosed is a synthesis suitable for large scale manufacture of an A 2A -adenosine receptor agonist, namely, (1-{9-[(4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminopurin-2-yl}pyrazol-4-yl)-N-methylcarboxamide. Also, disclosed are polymorphs of this compound and methods for isolating a specific polymorph. Also, disclosed are pharmaceutical compositions and methods for preparing pharmaceutical compositions.
1. A method of preparing a pharmaceutical composition comprising combining a monohydrate of the compound (1-{9-[(4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminopurin-2-yl}pyrazol-4-yl)-N-methylcarboxamide with at least one pharmaceutically acceptable carrier.
2. The method of claim 1 , wherein the pharmaceutically acceptable carrier comprises a buffered aqueous solution.
3. The method of claim 2 , wherein the monohydrate is a crystalline monohydrate that is substantially free of 2-hydrazinoadenosine.
4. The method of claim 3 , wherein the monohydrate is substantially free of other forms of the compound.
5. The method of claim 4 , wherein the monohydrate has a purity of at least about 99.6%.