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PREPARATION METHODS OF FORMS OF OPTICAL ENANTIOMERS OF MODAFINIL AND PHARMACEUTICAL COMPOSITION THEREOF
专利权人:
发明人:
申请号:
HK14105597.0
公开号:
HK1192220A
申请日:
2014.06.13
申请国别(地区):
HK
年份:
2014
代理人:
摘要:
Production of crystalline forms (specifically polymorphic forms or solvates) of enantiomers of modafinil (A) involves dissolving an enantiomer of (A) (preferably the levorotatory isomer, (-)-(A)) in a solvent other than ethanol, crystallizing the enantiomer and recovering the obtained crystalline form. Some polymorphic forms and solvates of (-)-(A) are new. Independent claims are included for: (a) the following new polymorphic forms of (-)-(A): (i) Form II, having an X-ray diffraction pattern with maxima corresponding to interplanar spacings of 8.54 Angstrom, 7.57 Angstrom, 7.44 Angstrom, 4.56 Angstrom, 3.78 Angstrom and 3.71 Angstrom (ii) Form III, having an X-ray diffraction pattern with maxima corresponding to interplanar spacings of 12.58 Angstrom, 8.54 Angstrom, 5.01 Angstrom, 4.10 Angstrom, 3.97 Angstrom and 3.20 Angstrom and (iii) Form IV, having an X-ray diffraction pattern with maxima corresponding to interplanar spacings of 12.38 Angstrom, 8.58 Angstrom, 7.34 Angstrom, 5.00 Angstrom and 4.09 Angstrom (b) a new dimethyl carbonate solvate of (-)-(A), having an X-ray diffraction pattern with maxima corresponding to interplanar spacings of 12.31 Angstrom, 9.69 Angstrom, 9.09 Angstrom, 8.54 Angstrom, 7.27 Angstrom, 6.21 Angstrom, 5.45 Angstrom, 5.10 Angstrom, 5.00 Angstrom, 4.83 Angstrom, 4.63 Angstrom, 4.46 Angstrom, 4.22 Angstrom, 4.21 Angstrom, 4.09 Angstrom, 3.78 Angstrom, 3.62 Angstrom, 3.53 Angstrom, 3.42 Angstrom, 3.32 Angstrom, 3.24 Angstrom, 3.21 Angstrom and 3.10 Angstrom (c) a method for converting a first crystalline form of an enantiomer of (A) (specifically Form I of (-)-(A)) into another crystalline form, involving suspending the first crystalline form in a suitable solvent and recovering the second form (the solvate specifically being acetonitrile, with the product being recovered as acetonitrile solvate) (d) a new acetonitrile solvate of (-)-(A), having an X-ray diffraction pattern with maxima corresponding to interplanar spacings of 16.17
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