Process for preparing an A2A-adenosine receptor agonist and its polymorphs
View Patent ↗Disclosed is a synthesis suitable for large scale manufacture of an A 2A -adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph.
1. A pharmaceutical composition prepared from a crystalline monohydrate form 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 by adding at least one pharmaceutically acceptable carrier.
2. The pharmaceutical composition of claim 1 , wherein the monohydrate is substantially free of 2-hydrazinoadenosine.
3. The pharmaceutical composition of claim 2 , wherein the monohydrate is substantially free of other hydrates or amorphous form.
4. The pharmaceutical composition of claim 3 , wherein the monohydrate has a purity of at least about 99.6%.
5. The pharmaceutical composition of claim 4 , wherein the monohydrate exhibits an X-ray powder diffraction pattern having peaks at diffraction angle 2θ (°) of about 6, about 9, about 11, about 13, about 14.5, about 16.5, and about 18 as measured by Cu-Kα1 X-ray powder diffractometry.