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IMPROVED PROCESS FOR THE PREPARATION OF STABLE CRYSTALLINE FORM-I OF LINEZOLID, SUBSTANTIALLY FREE OF RESIDUAL SOLVENT

机译:基本上不含残留溶剂的,稳定的线型唑啉晶体-I的制备方法得到改进

摘要

The invention relates to a substantially pure linezolid hydroxide having R-isomer content more than about 99.9% relative to its S-isomer. Further aspect of invention provides the ambient moisture condition, which is critical for enantiomeric pure linezolid hydroxide. The obtained substantially enantiomerically pure linezolid hydroxide compound of formula-II can be subsequently converted into the linezolid compound of formula-I, having S-isomer content more than 99.9% relative to R-isomer. Further the invention provides an improved process for preparation of enantiomeric pure linezolid Form-I, wherein linezolid Form-I having the purity more than 99.9% relative to any other known polymorphic form of linezolid. The obtained enantiomeric pure linezolid Form-I can be subsequently converted into the other known polymorphic forms linezolid. The invention also provides stable and substantially solvent-free crystal of Form-I of linezolid.
机译:本发明涉及一种相对于其S-异构体具有大于约99.9%的R-异构体含量的基本上纯的利奈唑烷。本发明的另一方面提供了环境湿度条件,这对于对映体纯的利奈唑烷氢氧化物是至关重要的。随后可以将所获得的基本上对映体纯的式II的利奈唑烷氢氧化物化合物转化成相对于R-异构体具有大于99.9%的S-异构体含量的式I的利奈唑烷化合物。此外,本发明提供了制备对映体纯的利奈唑胺形式I的改进方法,其中相对于利奈唑胺的任何其他已知多晶型形式,纯度高于99.9%的利奈唑胺形式I。所获得的对映体纯的利奈唑胺晶型I可随后转化为其他已知的多晶型物利奈唑胺。本发明还提供了利奈唑胺形式I的稳定且基本上无溶剂的晶体。

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