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Monday 27 July 2015

4-(4-Aminophenyl)-3-morpholinone a Rivaroxaban intermediate


ChemSpider 2D Image | 4-(4-Aminophenyl)-3-morpholinone | C10H12N2O2

4-(4-Aminophenyl)-3-morpholinone

  • Molecular FormulaC10H12N2O2
  • Average mass192.214 Da
438056-69-0 [RN]
T6NV DOTJ AR DZ [WLN]
4-(3-Oxo-4-morpholinyl)aniline
aminophenylmorpholinone
BR-26781
MFCD08236742 [MDL number]
ST-7900
mp 170-172 °C








see....http://www.google.com/patents/CN102746288A?cl=zh

4 - [(4- aminophenyl) _] 3- Morpholinone
[0039] 20g 4 - [(4- nitrophenyl) _] 3- morpholinone was dispersed in 200ml of ethanol was added 0.2g 5% palladium on carbon, at 0. 1MP50 ° C, the hydrogenation reaction was 8 hours, filtered and concentrated to one-half volume, (TC crystallization I hour, filtered and dried to yield 15. 5g white solid, yield 90% .


1H NMR (CDCl3):
7. 07 (d, 2H)   ortho to Ring
6 . 69 (d, 2H)  ortho to NH2
4. 32 (s, 2H)  OCH2C=0
4. 00 (t, 2H)
3. 72 (bs, 2H)
3. 69 (t, 2H)

1H NMR PREDICT







13C NMR PREDICT












Patents
The present invention relates to a process for preparing 4-(4-aminophenyl)-3- morpholinone by reacting ...
The invention belongs to the technical field of synthesis of 4-(4-aminophenyl)-3- morpholinone, and in particular relates to a novel synthetic ...
... reaction is effected in an aliphatic alcohol. In a specific embodiment, the 4-(4- aminophenyl)-3-morpholinone has the structure: (see formula I)
... carboxamide starting from 5-chlorothiophene-2-carbonyl chloride, (2S)-3- amino-propane-1,2-diol and 4-(4-aminophenyl)-3-morpholinone.
In this case, 2-[(2S)-2-oxiranylmethyl]-1H-isoindole-1,3(2H)dione (II) is reacted with 4-(4-aminophenyl)-3-morpholinone (III) to give ...
In this case, 2 - [(2S) -2-oxiranylmethyl] -lH-isoindole-l, 3 (2H) -dione (H) with 4- ( 4-aminophenyl) -3-morpholinone (Hl) to 2 - ((2R ) -2-hydroxy-3 ...
0 equivalents of 4- (4-aminophenyl) -3-morpholinone inorganic base as acid binding agent, with the water-immiscible organic solvent, a mixed ...
[0021] The present invention also provides a 3-morpholino-one and 4 - [(4- aminophenyl) -] 3- morpholinone of industrial production processes.

It provides process wherein, 2-[(2S)-2-oxiranylmethyl]-lH-isoindole-l,3(2H)dione ( II) is reacted with 4-(4-aminophenyl)-3-morpholinone (IE) to ...
4- (4-aminophenyl) -3-morpholinone (I) are prepared, the method is the following formula (11) 4- (4-nitrophenyl) morpholin-one as starting ...
US2007/0066611 relates to a process for preparing 4-(4-aminophenyl)-3- morpholinone by reacting 4-(4-nitrophenyl)-3-morpholinone with ...
... with 4- (4-Nitrophenyl) -3-morpholinone reduced to form the desired product 4- (4-aminophenyl) -3- morpholinone, the reaction conditions of ...
... I comprises the synthetic steps of taking 4-(4-aminophenyl)-3-morpholinone and 2-[(2S)-2-oxiranyl-methyl)-1H-isoindole-1,3(2H)-diketone as ...
... thiophene-2-carbonyl chloride, (2S)-3-amino-propane-l,2- diol and 4-(4- aminophenyl)-3-morpholinone. This synthesis uses toxic solvents or ...
[0012] This route substrate 4- (4-aminophenyl) -3-morpholinone 2_ compound with ethylene oxide reaction under reflux conditions in the ...
[0015] This route substrate 4- (4-aminophenyl) -3-morpholinone 2_ compound with ethylene oxide reaction under reflux conditions in the ...

... system crystallized to give 4 - (4-aminophenyl) -3-morpholinone; molar ratio of the iron powder and 4- (4-nitro-phenyl) -3-morpholinone is 2.
4-(4-aminophenyl)-3-morpholinone (38.5 g) was dissolved in a mixture of 400 ml of water and 400 ml of tetrahydrofuran at 45-50°C, then 32 ml ...
The rivaroxaban prepared according to the method of claim 1, characterized in that: said step a) 4- (4-aminophenyl) -3-morpholinone (11), 2- [ !
7,598,378 relates to a process for preparing 4-(4-aminophenyl)-3-morpholinone by reacting 4-(4-nitrophenyl)-3-morpholinone with hydrogen in ...
... and 4-(4-aminophenyl)-3- morpholinone. US 7,598,378 relates to a process for preparing 4-(4-aminophenyl)-3- morpholinone by reacting ...
[005] US 7,598,378, relates to a process for preparing 4-(4-aminophenyl)-3- morpholinone by ^ reacting 4-(4-nitrophenyl)-3-morpholinone with ...
US2007/0066611 relates to a process for preparing 4-(4-aminophenyl)-3- morpholinone by reacting 4-(4-nitrophenyl)-3-morpholinone with ...
... have been reported in many literatures 4- (4-aminophenyl) -3-morpholinone ( compound I) synthesis method, basically by first preparing 4- ...
[0019] 3-chloro-1,2-propanediol by cyclization, the reaction with phthalimide, then with 4- (4-aminophenyl) -3-morpholinone reaction, CDI and ...
US2007/0066611 relates to a process for preparing 4-(4-aminophenyl)-3- morpholinone by reacting. 4-(4-nitrophenyl)-3-morpholinone with ...
... acid methyl ester (example IB) was reacted with. 4-(4-amino-phenyl)-morpholin -3-one (CAS 438056-69-0) to ...
... Sep 9, 2004, Mar 24, 2005, Bayer Healthcare Ag, Method for the production of 4-(4-aminophenyl)-3-morpholinon.
... (example 1B) was reacted with 4- (4- amino-phenyl) -morpholin- 3- one (CAS 438056-69-0) to give 5-chloro-thiophene-2-carboxylic acid {(1S ...
... ester (example 1B) was reacted with 4-(4-amino-phenyl)-morpholin-3-one ( CAS 438056-69-0) to give 5-chloro-thiophene-2-carboxylic acid ...
... and 4- (4-aminophenyl) -3-morpholinone . This synthesis uses toxic solvents or reagents, which is dis¬ advantageous per se, and in addition ...
... reacting 2-[(2S)-2-oxiranylmethyl]-1 H-isoindole-1 ,3(2H)- dione with 4-(4- aminophenyl)-3-morpholinone to obtain 2-((2R)-2-hydroxy-3-{[4-(3- ...
... dione and 4- (4-aminophenyl) -3-morpholinone starting material for the method of preparing Rivaroxaban, which also relates to 4,.
... compounds 2-[(2S)-2-oxiranyl-methyl]-1-H-isoindole-1,3 (2H)-dione and 4-(4- aminophenyl)-3-morpholinone as starting materials, in which ...
... Sep 9, 2004, Mar 22, 2007, Bayer Healthcare Ag, Method for the production of 4-(4-aminophenyl)-3-morpholinone.
... 1B) and 4- (4-amino-3-fluoro - phenyl) - morpholin-3-one (CAS 438056-69-0) was obtained 5_ chloro - thiophene-2-carboxylic acid {(1S, 2S, ...
... 苯基)-吗啉-3-酮(CAS 438056-69-0)反应,得到3-{1(5-氯-噻吩-2-羰基)-氨基1-甲 基}-[1,2,4]噁二唑一5-曱酸14-(3-氧代-吗啉-4-基)-苯基卜酰胺。
And dried to give a white solid 10.2g, as Intermediate A, 92% molar yield (4- (4- aminophenyl) -3-morpholinone meter). [0061]实例2: [0061] ...
... reacted with 4-(4- amino-3-fluoro-phenyl)-morpholin-3-one (CAS 438056-69-0) to give 3-{ [(5-chloro- thiophene-2-carbonyl) -amino] -methyl}- ...
... reacted with 4-(4- amino-3-fluoro-phenyl)-morpholin-3-one (CAS 438056-69-0) to give 3-{ [(5-chloro- thiophene-2-carbonyl) -amino] -methyl}- ...



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