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US 12,162,815 B2Granted
Crystalline 2-fluoro-3-nitrotoluene and process for the preparation thereof
AssigneesF.I.S. Fabbrica Italiana Sintetici S.p.A., Amgen Inc.
InventorsElena Brasola, Marco Di Silvestro
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Abstract
The present invention refers to a crystalline 2-fluoro-3-nitrotoluene compound of formula (I), and a process for the preparation thereof. Furthermore, the present invention relates to a process for the synthesis of a compound of formula (II) or salts thereof by means of the crystalline 2-fluoro-3-nitrotoluene.
Claims17
A process for the synthesis of a compound of formula (II):
- or a salt thereof,
- wherein said process comprises the steps of:
- preparing crystalline 2-fluoro-3-nitrotoluene of formula (I):
- according to a process which comprises crystallization of the 2-fluoro-3-nitrotoluene of formula (I) from a mixture of water and a solvent selected from a C1-C3 alcohol, wherein the crystalline 2-fluoro-3-nitrotoluene of formula (I) has a DSC onset peak at a value among 25.0 and 26.0° C. or a DSC maximum peak at a value among 26.0 and 27.5° C. or an X-ray powder diffraction pattern comprising a peak expressed in 2-Theta values (2θ) at 14.3±0.2;
- and
- converting said crystalline 2-fluoro-3-nitrotoluene into the compound of formula (II), or a salt thereof.
3 more elements
Dependencies are inferred from the claim text.