cas 898543-06-1, (S)-4-(4-(5-(Aminomethyl)-2-oxooxazolidin-3-yl)phenyl)morpholin-3-one.HCl

Articles about 898543-06-1Total 20 be found

Article title
Article abstract
Author
Journal number and time
Download

Preparation of intermediates (by machine translation)
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)
-
Paragraph 0004; 0035-0037

(2020/10/19)

Preparation method of rivaroxaban intermediate
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.
-
(2019/12/25)

Preparation method and use of rivaroxaban intermediate
The present invention relates to a preparation method of a rivaroxaban intermediate I. The method provided by the invention has the advantages of greatly shortening the reaction time, easy preparationby scale, simple operation, good stability, high purity, low environmental pollution and suitable for industrial production.
-
(2019/04/26)

Preparation and application of key intermediate of rivaroxaban
The invention provides preparation and application of a key intermediate of rivaroxaban. Experiment conditions of a Gabriel method are optimized, and results show that a specific solvent is a key parameter which affects the purity and the yield of a rivaroxaban intermediate. The rivaroxaban prepared by the invention is high in yield and good in purity, and is capable of meeting quality standards of raw material medicines without recrystallization.
-
Paragraph 0034; 0037-0042

(2019/09/14)

An Improved Synthesis of Rivaroxaban
-
Tian, Shaixiao,Tang, Bo,Zhang, Minzhong,Gao, Qingjiao,Chen, Bo,Zhang, Qinghua,Xu, Guangyu
p. 169 - 177
(2017/04/26)

4 - (4 - a ammonia alkenyl phenyl) - 3 - morpholone and its preparation method
The present invention discloses a compound 4-(4-methylamino alkenyl phenyl)-3-morpholinone represented by a formula III, and a preparation method thereof. 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 operation of the preparation method is simple, the yield is up to about 90%, and the product purity is good. The formula III is defined in the specification.
-
(2017/08/25)

A method for synthesizing [...] (by machine translation)
The invention discloses a method for synthesizing [...], from 4 - (4 - a ammonia alkenyl phenyl) - 3 - morpholone with (S)- {1 - (chloromethane ester) - 2 - [2 - (1, 3 - two oxygen different indole) yl] ethyl} halide salt to ring-closure reaction, to make the key intermediate (S)- 2 - {[2 - oxo - 3 - (4 - (3 - oxo-morpholine) phenyl) oxazolidine - 5 - yl] methyl} isoindole - 1, 3 - dione, then the key intermediate to remove the amino protecting base 4 - {4 - [(5 S) - 5 - (aminomethyl) - 2 - oxo - 1, 3 - oxazolidine - 3 - yl] phenyl} morpholine - 3 - one hydrochloride, with 2 - chloro formyl - 5 - [...][...] further reaction. This invention prepares mild condition, the process is simple, low cost, high yield, is suitable for industrial production. (by machine translation)
-
(2018/04/01)

A process for preparing 4 - (4 - aminophenyl) - 3 - morpholinon method (by machine translation)
The invention discloses a process for preparing 4 - (4 - aminophenyl) - 3 - morpholone (type IV) method, which belongs to the field of chemical synthesis. The specific method comprises: intermediate N - (4 - aminophenyl) - 2 - (2 - halo ethoxy) acetamide (type III) by the one-step cyclization reaction systems benefit cuts down Sha Ban key intermediate 4 - (4 - aminophenyl) - 3 - morpholone (type IV), wherein X represents halogen. The prepared 4 - (4 - aminophenyl) - 3 - morpholinon purity is good, the reaction yield is high, can be as high as 87% of the left and right, and the preparation process avoids the use of expensive metal palladium on nitro reduction, the operation is simple, and is suitable for industrial production. (by machine translation)
-
(2017/08/24)

(S)- {1 - (chloromethane ester) - 2 - [2 - (1, 3 - two oxygen different indole) yl] ethyl} halide salt and its preparation method
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.
-
Paragraph 0102-0104

(2017/08/25)

NOVEL MORPHOLINE DIPHOSPHATE SALT, AND METHOD FOR MANUFACTURING HIGH PURITY RIVAROXABAN USING SAME
The present invention relates to a method of producing 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophene carboxamide (hereinafter, andPrime;rivaroxabanandPrime;, chemical formula 1) with high purity in an economical and mass-producible manner by using novel 4-{4-[(5S)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl}morpholine-3-one disphosphate salts (hereinafter, andPrime;morpholine disphosphate saltsandPrime;, chemical formula 2).COPYRIGHT KIPO 2017
-
Paragraph 0058-0063

(2017/12/15)

A method for the preparation of key intermediate the advantage cuts down Sha Ban
The invention relates to a preparation method of a rivaroxaban key intermediate, particularly a preparation method of 4-[4-[(5S)-5-(aminomethyl)-2-oxo-3-oxazolidinyl]phenyl]-3-morpholone hydrochloride (compound 4), which comprises the following steps: reacting dibenzyl ammonia with R-epoxy chloropropane to obtain N,N-dibenzyl epoxypropane (compound 1), reacting the compound 1 with 4-(4-aminophenyl)morpholinyl-3-one to obtain a compound 2, reacting the compound 2 with N,N-carbonyl-diimidazole to obtain a compound 3, and catalyzing the compound 3 with palladium on carbon to obtain the 4-[4-[(5S)-5-(aminomethyl)-2-oxo-3-oxazolidinyl]phenyl]-3-morpholone hydrochloride.
-
Paragraph 0020; 0047; 0048; 0049; 0050

(2017/08/25)

4 - (nitro-phenyl) - 3-preparation of morpholinones the advantage cuts down Sha Ban method and using the same method of preparation
The invention relates to the technical field of preparation of rivaroxaban and an intermediate thereof and particularly relates to a preparation method of 4-(nitrobenzophenone)-3-morpholone which is prepared from halogenated nitrobenzene, ethanolamine and chloroacetyl chloride through a one-pot method. The method for preparing rivaroxaban comprises the steps of reducing 4-(nitrobenzophenone)-3-morpholone into 4-(aminophenyl)-3-morpholone; enabling 4-(aminophenyl)-3-morpholone to react with R-epichlorohydrin to obtain a product; enabling the product to react with N, N-carbonyldiimidazole to obtain a product; enabling the product to react with tert-butyl iminodicarboxylate; preparing hydrochloride; enabling hydrochloride to react with 5-penphene-2-carbonyl chloride. The preparation method of 4-(nitrobenzophenone)-3-morpholone is capable of realizing one-pot production and free of purifying intermediate products in the process, so that the operation process is simplified, the time is saved, and the labor cost is reduced; the preparation method of 4-(nitrobenzophenone)-3-morpholone is low in raw material price, high in obtained product yield and easy to realize large-scale industrial production; in addition, the method for preparing rivaroxaban is cheap, nontoxic and harmless in raw material, simple in process and high in product yield.
-
(2017/02/02)

PROCESS FOR THE PREPARATION OF RIVAROXABAN
Disclosed is a process for the preparation of rivaroxaban and purifying rivaroxaban.
-
Paragraph 0130; 0150

(2016/06/01)

PROCESS FOR PREPARATION OF RIVAROXABAN AND INTERMEDIATES THEREOF
An improved process for the preparation of Rivaroxaban wherein the process substantially eliminates the potential impurities. process for preparation of Rivaroxaban which uses a novel intermediate. A process for preparing the novel intermediate which is used for the preparation of Rivaroxaban.
-
(2015/02/18)

RIVAROXABAN INTERMEDIATE AND PREPARATION THEREOF
This invention relates to novel intermediate, formula (A) for rivaroxaban and process for the preparation thereof. Further it extends to the process for preparation of rivaroxaban by using the said novel intermediate, by treating with 5-chlorothiophene carbonyl chloride to form the rivaroxaban derivatives of formula (B). The obtained formula (B) further treated with acid to form rivaroxaban.
-
(2014/07/21)

PROCESSES FOR THE PREPARATION OF 5-CHLORO-N-({(5S)-2-OXO-3-[4-(3-OXO-4-MORPHOLINYL) PHENYL]-1,3-OXAZOLIDIN-5-YL}METHYL)-2-THIOPHENE-CARBOXAMIDE AND INTERMEDIATES THEREOF
TThe present invention provides processes for the preparation of 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophene-carboxamide (I) and intermediates thereof. Also provides novel intermediates and their use in the synthesis of oxazolidine derivatives.
-
(2013/04/13)

PROCESS FOR PREPARING FACTOR XA INHIBITORS
The present invention relates to a process for the manufacturing of a rivaroxaban or a pharmaceutically acceptable salt thereof, wherein the process comprises obtaining an acid addition salt of a 4-{4-[(5S))-5-(aminomethyl)-2-oxo-1,3-oxozoladine-3- yl]phenyl}morpholin-3-one, and reacting the acid addition salt with the suitable reagents to obtain rivaroxaban or a salt thereof.
-
(2013/04/25)

A PROCESS FOR PREPARATION OF RIVAROXABAN AND INTERMEDIATES THEREOF
An improved process for the preparation of Rivaroxaban; wherein the said process substantially eliminates the potential impurities. The present invention also relates to process for preparation of Rivaroxaban using a novel intermediate. The present invention also relates to a process for preparing the novel intermediate, used for preparation of Rivaroxaban.
-
(2013/08/28)

METHOD FOR THE PREPARATION OF SUBSTITUTED OXAZOLIDINONES
The present invention relates to methods for the preparation of a compound having the formula (X). Individual reaction steps as welt as intermediates are additionally claimed.
-
Page/Page column 30

(2012/11/06)

PROCESS FOR DETERMINING THE SUITABILITY FOR DISTRIBUTION OF A BATCH OF A THIOPHENE-2-CARBOXAMIDE DERIVATIVE
The present invention relates to a process for determining the suitability for distribution of a batch of rivaroxaban or of a pharmaceutical composition thereof. In particular, it also relates to two impurities of rivaroxaban, to their use as reference markers to determine the purity of a sample of rivaroxaban or a composition thereof, to analytical methods for determining the purity of a sample of rivaroxaban or a composition thereof and to a process of preparing rivaroxaban or pharmaceutical compositions thereof which are free or substantially free of such impurities.
-
Page/Page column 29

(2012/04/04)