Tetrahedron Letters p. 99 - 101 (2019)
Update date:2022-08-17
Topics:
Drabina, Pavel
Feixová, Viola
Sedlák, Milo?
A new synthetic approach towards the anticoagulant drug (S)-Rivaroxaban was described. This reaction sequence involved six steps overall, starting from commercially available and inexpensive N-(4-aminophenyl)morpholin-3-one. The stereogenic centre was introduced by an asymmetric Henry reaction catalysed by the complex of copper(II) acetate and (2R,5S)-2-(pyridine-2-yl)imidazolidine-4-one with 87% ee. The individual reaction steps proceeded with high yields and did not require any unusual or expensive reagents.
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