| 摘要 |
In the present invention, there is disclosed a polymorph of 2-[4-[(methylamino)carbonyl]-1H-pyrazol-1-yl]adenosine (designated as polymorph E), characterized by X-ray diffractogram X-RPD exhibiting reflections at 2 {theta} = 5.8 degree, 12.3 degree, 15.9 degree, 17.3 degree, 20.5 degree, 22.6 degree, 23.6 degree, 27.7 degree and 29.2 degree and further characterized by means of DSC, where it exhibit a significant endothermic transition in the range of 258 to 264 degC, and further characterized by means of IR spectrum. The E polymorph is prepared in a process comprising the following operations: a) mixing of 2-[4-[(methylamino)carbonyl]-1H-pyrazol-1-yl]adenosine with a polar aprotic solvent, preferably with dimethylsulfoxide, and heating thereof to obtain a saturated solution; b) cooling the saturated solution to obtain a turbid solution of 2-[4-[(methylamino)carbonyl]-1H-pyrazol-1-yl]adenosine; c) adding the turbid solution of the 2-[4-[(methylamino)carbonyl]-1H-pyrazol-1-yl]adenosine into a protic solvent, preferably methanol, under simultaneous precipitation of a jellylike precipitate; d) heating the precipitated jellylike precipitate in a protic solvent up to boil to obtain polymorph E suspension and; e) cooling the suspension, isolation of drying the polymorph E. |
