CRYSTALLINE FORM OF PYRIMIDIO[6,1-A]ISOQUINOLIN-4-ONE COMPOUND

The current invention is directed towards a polymorph of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H -pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, in the form of a crystalline solid consisting of greater than 99% by weight of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6...

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Hauptverfasser: MICHAEL JOHN ALFRED WALKER, BERTRAND MICHEL CLAUDE PLOUVIER, JULIAN S. NORTHEN, PHILIPPE FERNANDES
Format: Patent
Sprache:eng ; spa
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Zusammenfassung:The current invention is directed towards a polymorph of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H -pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, in the form of a crystalline solid consisting of greater than 99% by weight of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H -pyrimido[6,1-a]-isoquinoIin-3(4H)-yl]ethyl}urea, at least 95% in the polymorphic form of a thermodynamically stable polymorph (I) of N-{2-[(2E)-2-(mesitylimino)-9,10-dimetlioxy-4-oxo-6,7-dihydro-2 H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, wherein said polymorph is determined by single crystal X-ray structural analysis and X-ray powder diffraction pattern. La presente invención está dirigida hacia un polimorfo de N-{2-[(2E)-2-(mesitilimino)-9, 10-dimetoxi-4-oxo-6 7-dihidro-2H-pirimido [6, 1-a]-isoquinolin-3(4H)-il] etilo}urea, en la forma de un sólido cristalino que consiste de más de 99% por peso de N-{2-[(2E)-2-(mesitilimino)-9,10-dimetoxi-4-oxo-6, 7-dihidro-2H-pirimido [6, 1-a]-isoquinolin-3(4H)-il]etilo}urea, por lo menos 95 en la forma polimórfica de un polimorfo (1) termodinámicamente estable de N-{2-[(2E)-2-(mesitilimino) -9,10-dimetoxi-4-oxo-6, 7-dihidro-2H-pirimido [6, 1-a]-isoquinolin-3(4H)-il] etilo}urea, en donde el polimorfo es determinado por el análisis estructural de Rayos X del monocristal y patrón de difracción de polvo de rayos X.