869785-51-3Relevant articles and documents
Facile preparation of 4-(4-nitrophenyl)morpholin-3-one via the acid-catalyzed selective oxidation of 4-(4-nitrophenyl)morpholine by sodium chlorite as the sole oxidant
Chu, Changhu,Jia, Qiang,Liu, Chaoyang,Qin, Cheng,Sun, Haozhou,Yang, Tiannuo,Yu, Tao
, p. 2633 - 2638 (2020)
4-(4-Nitrophenyl)morpholin-3-one and 4-(4-aminophenyl) morpholin-3-one are the key intermediates for rivaroxaban synthesis. A facile and economically efficient process has been developed for the preparation of these intermediates. Excellent yield of 4-(4-nitrophenyl)morpholine is obtained by condensing 4-chloro nitrobenzene and morpholine, and 4-(4- nitrophenyl)morpholine is oxidized using inexpensive sodium chlorite to achieve a good yield of the corresponding 4-(4- nitrophenyl)morpholin-3-one. Finally, the key intermediate of rivaroxaban, 4-(4-aminophenyl) morpholin-3-one, is achieved by the iron(III)-catalyzed reduction of the nitro group with aqueous hydrazine. No high-cost materials were used, and the process did not require column purification.
NOVEL SUBSTITUTED THIOPHENECARBOXAMIDES, THEIR PRODUCTION AND THEIR USE AS MEDICAMENTS
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Page/Page column 166-167, (2008/06/13)
The invention relates to novel substituted thiophene-2-carboxamides of general formula (I), in which A, and R1 to R8c are defined as cited in claim 1. The invention also relates to the tautomers, enantiomers, diastereomers, mixtures and salts, in particular the physiologically compatible salts of said compounds containing inorganic or organic acids or bases, which exhibit valuable properties.