The invention provides synthetic methods of related substances F and G of rivaroxaban. With the adoption of the synthetic methods of the related substances F and G of the rivaroxaban, the yield is high, and industrial production and technology transformation are realized easily.
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Paragraph 0085-0089; 0092; 0095
(2018/03/01)
A oxazolidinone compounds of preparation method
The invention discloses a method for preparing an oxazolidinone compound. The method comprises the following steps of carrying out ammonolysis reaction on a racemic or optically active 3-chloro-2-hydroxypropyl aniline compound (2) as a starting material and ammonia in a proper solvent and under alkaline condition to obtain a 3-amino-2-hydroxypropyl aniline compound (3); carrying out acylation reaction on the compound (3) to obtain 3-acylamino-2-hydroxypropyl aniline compound (4); and carrying out cyclization reaction on the compound (4) and a corresponding acylating reagent to obtain the racemic or optically active oxazolidinone compound (II) as shown in the description, wherein R1 represents morpholinyl or 3-oxo-4-morpholinyl; R2 represents H or F; and R3 represents C1-12 alkyl, 5-chloro-thiophen-2-yl, thiophen-2-yl or 4,5-dichloro-2-yl; and the compound is a racemate and (S)- or (R)- optical isomers.