Farmak, A.s.

Barbora Dvorakova

Pavel Hradil

Lubomir Kvapil

Petr Slezar

Martin Grepl

The invention relates to a compound which is, 2-[4-[(methylamino)carbonyl]-1H-pyrazol-1-yl]adenosine, which is a selective A2A adenosine receptor agonist in myocardial imaging. The new polymorph of 2-[4-[(methylamino)carbonyl]-1H-pyrazol-1-yl]adenosine (designated as polymorph E) is characterized by an X-ray diffraction pattern of X-RPD showing the following reflections at 2 Theta=5.8&#xb0;, 12.3&#xb0;, 15.9&#xb0;, 17.3&#xb0;, 20.5&#xb0;, 22.6&#xb0;, 23.6&#xb0;, 27.7&#xb0;, and 29.2&#xb0;; and further characterized by a DSC scan showing marked endotherm in the range of 258 to 264&#xb0; C.; and further characterized by a specific IR spectra. The invention further relates to a method of preparing the polymorph by recrystallization from other polymorphic forms of 2-[4-[(methylamino)carbonyl]-1H-pyrazol-1-yl]adenosine by a procedure comprising the following operations: mixing of 2-[4-[(methylamino)carbonyl]-1H-pyrazol-1-yl]adenosine with a polar aprotic solvent, preferably with dimethylsulfoxide, and heating to form a saturated solution; cooling of the saturated solution with formation of a turbid solution of 2-[4-[(methylamino)carbonyl]-1H-pyrazol-1-yl]adenosine; addition of the turbid solution of 2-[4-[(methylamino)carbonyl]-1H-pyrazol-1-yl]adenosine to a protic solvent, preferably methanol, with separation of a gel-like precipitate; heating of the separated gel-like precipitate in the protic solvent to a boil with formation of a suspension of polymorph E; and cooling of the suspension, isolation and drying of polymorph E.

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Barbora Dvorakova