898543-06-1Relevant articles and documents
Preparation of intermediates (by machine translation)
-
Paragraph 0004; 0035-0037, (2020/10/19)
In the method of manufacturing a method of manufacturing problems [to] [ribarokisaban[ribarokisaban][ribarokisaban[ribarokisaban] which, in particular, intermediate compounds on an industrial scale manufacturing method is excellent in operability. [Solution] water-miscible organic solvent other than alcohols in, 2 - ({(5S) -2 - [4 - (3 - oxo--4 - morpholinyl) - phenyl] - 1, 3 - oxazolidine -3 - oxo -5 - yl} methyl) - 1, 3 (2H) dione is reacted with methylamine - 1H - isoindole, 2 layers separated from the solution 4 - {4 - [(aminomethyl) - 1, 3 - oxazolidine -3 - oxo (5S) -5 - -2 - yl] - phenyl} morpholine hydrochloride is precipitated on the production of -3 -, and method of manufacturing the compound [ribarokisaban[ribarokisaban]. Figure 4 [drawing] (by machine translation)
Preparation method of rivaroxaban intermediate
-
, (2019/12/25)
The invention discloses a preparation method of a Rivaroxaban intermediate. The preparation method includes the following steps that (1) in existence of an organic lithium salt or the organic lithiumsalt and an inorganic lithium salt, a compound in a following formula I is reacted with a compound in a following formula II to obtain a compound in a following formula III; and (2) the compound in the formula III is subjected to an acidification reaction in existence of inorganic acid HX, the Rivaroxaban intermediate shown in a following formula IV is obtained, wherein R in the compound in the formula I is selected from methyl, isopropyl, normal-butyl and phenyl or benzyl, and the inorganic acid HX is selected from hydrochloric acid or sulfuric acid. The preparation method is easy to operateand high in yield, and industrial production and patent medicine quality control are convenient.
(S)- {1 - (chloromethane ester) - 2 - [2 - (1, 3 - two oxygen different indole) yl] ethyl} halide salt and its preparation method
-
Paragraph 0102-0104, (2017/08/25)
The present invention discloses a compound (S)-{1-(chloroformate)-2-[2-(1,3-dioxo-isoindol)yl]ethyl}halogenation salt represented by a formula VI, and a preparation method thereof, wherein X represents a halogen. According to the present invention, the compound is used for preparing the rivaroxaban key intermediate (S)-2-{[2-oxo-3-(4-(3-oxomorpholino)phenyl)oxazolidine-5-yl]methyl}isoindole-1,3-dione and/or rivaroxaban intermediate, and the obtained product is firstly obtained through the method in the present invention; and the preparation method is mature and reliable, and can be suitable for industrial large-scale production. The formula VI is defined in the specification.