149141-11-7Relevant articles and documents
Intermediate for preparing pexidartinib, and preparation method and application thereof
-
Paragraph 0069-0072; 0073-0076, (2020/07/12)
The invention discloses an intermediate for preparing pexidartinib, a preparation method and application thereof. According to the invention, raw materials and reagents used in the method are cheap and easily available, the ultralow-temperature reaction and corrosive trifluoroacetic acid are successfully avoided, the method has low requirements on equipment and is beneficial to energy conservationand emission reduction, the preparation process of pexidartinib and related intermediates is simple to operate, post-treatment and purification are convenient, column chromatography is not needed, and the total yield is up to 48%; according to the method, a compound (IV) is prepared from a compound (II), a compound (V) is prepared from a compound (IV), and pexidartinib is prepared, so that the defects and deficiencies of preparation methods reported in literatures are overcome; and the intermediate for preparing pexidartinib is a compound with a structure represented by a formula (A1), a compound with a structure represented by a formula (II) or a compound with a structure represented by a formula (IV).