2-[(2R)-2-Hydroxy-3-[[4-(3-oxo-4-Morpho linyl)phenyl]aMino]propyl]-1H-isoindole-1 ,3(2H)-dione

Product Name: 2-[(2R)-2-Hydroxy-3-[[4-(3-oxo-4-Morpho linyl)phenyl]aMino]propyl]-1H-isoindole-1 ,3(2H)-dione
CAS No.: 446292-07-5
Chemical Name: 2-[(2R)-2-Hydroxy-3-[[4-(3-oxo-4-Morpho linyl)phenyl]aMino]propyl]-1H-isoindole-1 ,3(2H)-dione
Synonyms: C21H2IN3Os .;2-Amino-12-picoline;Rivaroxaban Impurity 50;Rivaroxaban interMediate B;Rivaroxaban Intermediates I;Intermediate of Rivaroxaban 4;Rivaroxaban Phthalimido Analog;-2-(2-Hydroxy-3-((4-(3-oxomorpholino);Rivaroxaban Phthalimido Descarbonyl Impurity;Rivaroxaban Phthalamide [oxazolidone ring opend] impurity
CBNumber: CB12468597
Molecular Formula: C21H21N3O5
Formula Weight: 395.41
MOL File: 446292-07-5.mol

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2-[(2R)-2-Hydroxy-3-[[4-(3-oxo-4-Morpho linyl)phenyl]aMino]propyl]-1H-isoindole-1 ,3(2H)-dione Property

Melting point:: 208-211°C
Boiling point:: 734.9±60.0 °C(Predicted)
Density: 1.421
storage temp.: under inert gas (nitrogen or Argon) at 2–8 °C
solubility: DMSO (Slightly), Methanol (Slightly, Heated)
pka: 13.91±0.20(Predicted)
form: Solid
color: White to Off-White
Water Solubility: 37mg/L at 20℃
InChI: InChI=1S/C21H21N3O5/c25-16(12-24-20(27)17-3-1-2-4-18(17)21(24)28)11-22-14-5-7-15(8-6-14)23-9-10-29-13-19(23)26/h1-8,16,22,25H,9-13H2/t16-/m1/s1
InChIKey: CKFVSMPWXAASIQ-MRXNPFEDSA-N
SMILES: C1(=O)C2=C(C=CC=C2)C(=O)N1C[C@H](O)CNC1=CC=C(N2CCOCC2=O)C=C1
LogP: 0.6 at 25℃
CAS DataBase Reference: 446292-07-5

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Safety

HS Code: 2922498590

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H312Harmful in contact with skin

H332Harmful if inhaled

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P322Specific measures (see …on this label).

P330Rinse mouth.

P363Wash contaminated clothing before reuse.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

TRC

Product number: H948920
Product name: 4-[((2R)-Hydroxy-3-phthalimido)propylamine]phenyl-3-morpholinone
Packaging: 25mg
Price: $385
Updated: 2021/12/16

TRC

Product number: H948920
Product name: 4-[((2R)-Hydroxy-3-phthalimido)propylamine]phenyl-3-morpholinone
Packaging: 50mg
Price: $725
Updated: 2021/12/16

AK Scientific

Product number: Z3537
Product name: 2-[(2R)-2-Hydroxy-3-[[4-(3-oxo-4-mopholinyl)phenyl]amino]propyl]-1H-isoindole-1,3(2h)-dione
Packaging: 100mg
Price: $82
Updated: 2021/12/16

American Custom Chemicals Corporation

Product number: CCH0032813
Product name: (R)-2-(2-HYDROXY-3-((4-(3-OXOMORPHOLINO)PHENYL)AMINO)PROPYL)ISOINDOLINE-1,3-DIONE
Purity: 95.00%
Packaging: 1G
Price: $402.15
Updated: 2021/12/16

AK Scientific

Product number: Z3537
Product name: 2-[(2R)-2-Hydroxy-3-[[4-(3-oxo-4-mopholinyl)phenyl]amino]propyl]-1H-isoindole-1,3(2h)-dione
Packaging: 1g
Price: $139
Updated: 2021/12/16

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2-[(2R)-2-Hydroxy-3-[[4-(3-oxo-4-Morpho linyl)phenyl]aMino]propyl]-1H-isoindole-1 ,3(2H)-dione Chemical Properties,Usage,Production

Chemical Properties

White Solid

Uses

4-[((2R)-Hydroxy-3-phthalimido)propylamine]phenyl-3-morpholinone is a Rivaroxaban (R538000(P)) intermediate. Rivaroxaban is a novel antithrombotic agent. It is also a highly potent and selective, direct FXa inhibitor.

Uses

Rivaroxaban intermediate.

Flammability and Explosibility

Non flammable

Synthesis

1252018-10-2

1074-82-4

446292-07-5

Example 3: Preparation of (R)-2-(2-hydroxy-3-((4-(3-oxomorpholinyl)phenyl)amino)propyl)isoindoline-1,3-dione (7a): phthalimide potassium salt (7.16 g, 38.632 mmol) was added in a single addition to a mechanically stirred N,N-dimethylformamide (DMF, 60 mL) solution of 4-[4-(N-(3-chloro-2R-hydroxy-1-propyl)amino)phenyl]morpholine -3-one (10 g, 35.119 mmol) in a solution of N,N-dimethylformamide (DMF, 60 mL). After stirring the suspension at room temperature, it was heated to 100 °C and stirred continuously at this temperature for 3 hours. After the reaction was completed, the mixture was cooled to room temperature. Water (60 mL) was added and the suspension continued to be stirred for 15 minutes. Subsequently, the suspension was filtered through a Brinell funnel and the solid product was collected. The solid was washed with distilled water (2 x 40 mL) and dried under vacuum at 50 °C for 10 h to afford the target product (R)-2-(2-hydroxy-3-((4-(3-oxomorpholinyl)phenyl)amino)propyl)isoindoline-1,3-dione (12.55 g, 93% yield) as a white crystalline solid.1H NMR (400 MHz, DMSO-d6) δ. 2.99-3.05 (m, 1H), 3.14-3.2 (m, 1H), 3.59-3.69 (m, 4H), 3.91-3.94 (m, 2H), 3.97-4.05 (m, 1H), 4.14 (s, 2H), 5.16 (d, J = 5.2 Hz, 1H), 5.66 (t, J = 6.0 Hz, 1H), 6.61 (d, J = 6.0 Hz, 1H), 6.61 (d, J = 6.0 Hz, 1H). 6.61 (d, J = 8.7 Hz, 2H), 7.03 (d, J = 8.8 Hz, 2H), 7.82-7.88 (m, 4H).

References

[1] Patent: WO2012/51692, 2012, A1. Location in patent: Page/Page column 42-43
[2] Patent: CN103951661, 2017, B. Location in patent: Paragraph 0043-0044
[3] Patent: CN104974105, 2017, B. Location in patent: Paragraph 0073
[4] Patent: CN104974149, 2018, B. Location in patent: Paragraph 0074; 0075; 0077; 0081; 0083
[5] Patent: WO2012/32533, 2012, A2. Location in patent: Page/Page column 15

2-[(2R)-2-Hydroxy-3-[[4-(3-oxo-4-Morpho linyl)phenyl]aMino]propyl]-1H-isoindole-1 ,3(2H)-dione Preparation Products And Raw materials

Raw materials

Preparation Products

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2-[(2R)-2-Hydroxy-3-[[4-(3-oxo-4-Morpho linyl)phenyl]aMino]propyl]-1H-isoindole-1 ,3(2H)-dione Suppliers

Canada 1 China 241 India 16 United Kingdom 2 United States 9 Global 269

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View Lastest Price from 2-[(2R)-2-Hydroxy-3-[[4-(3-oxo-4-Morpho linyl)phenyl]aMino]propyl]-1H-isoindole-1 ,3(2H)-dione manufacturers

Henan Aochuang Chemical Co.,Ltd.

Product: 1H-ISOINDOLE-1,3(2H)-DIONE, 2-[(2R)-2-HYDROXY-3-[[4-(3-OXO-4-MORPHOLINYL)PHENYL]AMINO]PROPYL]- 446292-07-5
Price: US $0.00-0.00/kg
Min. Order: 1kg
Purity: 98%
Supply Ability: 1Ton
Release date: 2022-09-19

Anhui Dexinjia Biopharm Co., Ltd

Product: 2-[(2R)-2-Hydroxy-3-[[4-(3-oxo-4-Morpho linyl)phenyl]aMino]propyl]-1H-isoindole-1 ,3(2H)-dione 446292-07-5
Price: US $100.00-2500.00/KG
Min. Order: 1KG
Purity: 99%
Supply Ability: 2MT per month
Release date: 2023-12-26

Changzhou Rokechem Technology Co., Ltd.

Product: 2-[(2R)-2-HYDROXY-3-[[4-(3-OXO-4-MORPHOLINYL)PHENYL]AMINO]PROPYL]-1H-ISOINDOLE- 1,3(2H)-DIONE 446292-07-5
Price: US $0.00-0.00/Kg
Min. Order: 1Kg
Purity: 99%
Supply Ability: 1-10000kgs
Release date: 2023-05-25

446292-07-5, 2-[(2R)-2-Hydroxy-3-[[4-(3-oxo-4-Morpho linyl)phenyl]aMino]propyl]-1H-isoindole-1 ,3(2H)-dioneRelated Search:

1,2-BenzenedicarboxaMide, N1,N2-bis[[(5S)-2-oxo-3-[4-(3-oxo-4-Morpholinyl)phenyl]-5-oxazolidinyl]Methyl]- 2-QuinazolineMethanol, 4-Methyl- Rivaroxaban Impurity 34 (R)-N-Glycidylphthalimide 4,5-DICHLOROTHIOPHENE-2-CARBOXYLIC ACID 2-Thiophenecarboxylic acid 1H-ISOINDOLE-1,3(2H)-DIONE, 2-[[(5S)-2-OXO-3-[4-(3-OXO-4-MORPHOLINYL)PHENYL]-5-OXAZOLIDINYL]METHYL]- Rivaroxaban POLYSTYRENE IODOSOACETATE 1,2-Cyclohexanedione 4-(4-NITROPHENYL)MORPHOLIN-3-ONE (S)-(+)-Glycidyl Phthalimide 4-[4-(N-(3-chloro-(2R)-2-hydroxy-1-propyl)aMino)phenyl]Morpholin-3-one (S)-4-(4-(5-(Aminomethyl)-2-oxooxazolidin-3-yl)phenyl)morpholin-3-one.HCl 5-CHLOROTHIOPHENE-2-CARBONYL CHLORIDE Ethyl (R)-(-)-4-cyano-3-hydroxybutyate 3-MORPHOLINONE, 4-[4-[(5S)-5-(AMINOMETHYL)-2-OXO-3-OXAZOLIDINYL]PHENYL]- (S)-(+)-Epichlorohydrin

Rivaroxaban Impurity 10/4-[((2R)-Hydroxy-3-phthalimido)propylamine]phenyl-3-morpholinone

1H-ISOINDOLE-1,3(2H)-DIONE, 2-[(2R)-2-HYDROXY-3-[[4-(3-OXO-4-MORPHOLINYL)PHENYL]AMINO]PROPYL]-

4-[((2R)-Hydroxy-3-phthaliMido)propylaMine]phenyl-3-Morpholinone

2-[(2R)-2-Hydroxy-3-[[4-(3-oxo-4-morpholinyl)phenyl]amino]propyl]-1H-isoindole-1,3(2H)-dione

2-[(2R)-2-hydroxy-3-{[4-(3-oxoMorpholin-4-yl)phenyl]aMino}p ropyl]-1H-isoindole-1,3(2H)-dione

(R)-2-(2-Hydroxy-3-((4-(3-oxomorpholino)phenyl)-amino)propyl)isoindoline-1,3-dione

Rivaroxaban interMediate B

2-[(2R)-2-hydroxy-3-[4-(3-oxomorpholin-4-yl)anilino]propyl]isoindole-1,3-dione

Rivaroxaban Phthalimido Descarbonyl Impurity

2-[(2R)-2-HYDROXY-3-[[4-(3-OXO-4-MORPHOLINYL)PHENYL]AMINO]PROPYL]-

-2-(2-Hydroxy-3-((4-(3-oxomorpholino)

Rivaroxaban Impurity 50

H-ISOINDOLE-1,3(2H)-DIONE, 2-[(2R)-2-HYDROXY-3-[[4-(3-OXO-4-MORPHOLINYL)PHENYL]AMINO]PROPYL]-

R –(2-Hydroxy-3-((4-(3-Oxo morpholino) Phenyl) Amino) Propyl) Isoindoline-1,3-dione

2-Amino-12-picoline

2-[(2R)-2-hydroxy-3-{[4-(3-oxomorpholin-4-yl)phenyl]amino}pr...

TIANFUCHEM--446292-07-5---1H-ISOINDOLE-1,3(2H)-DIONE, 2-[(2R)-2-HYDROXY-3-[[4-(3-OXO-4-MORPHOLINYL)PHENYL]AMINO]PROPYL]-

C21H2IN3Os .

Intermediate of Rivaroxaban 4

Rivaroxaban Intermediates I

(R)-2-{2-Hydroxy-3-[4-(3-oxo-morpholin-4-yl)-phenylamino]-propyl}-isoindole-1,3-dione

Rivaroxaban Phthalimido Analog

2-[(2R)-2-Hydroxy-3-[4-(3-oxo-mprpholinyl)phenyl]aminopropyl]-1H-isoindole-1,3-(2H)-dione

Rivaroxaban Phthalamide [oxazolidone ring opend] impurity

2-[(2R)-2-Hydroxy-3-[[4-(3-oxo-4-Morpho linyl)phenyl]aMino]propyl]-1H-isoindole-1

(R)-2-(2-Hydroxy-3-((4-(3-oxomorpholino)phenyl)amino)propyl)isoindoline-1,3-dione (Intermediate of Rivaroxaban)

446292-07-5

Chiral Reagents

Heterocycles

Intermediates & Fine Chemicals

Pharmaceuticals

Intermediate of Rivaroxaban