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956104-40-8

  • Product Name:Apalutamide
  • Molecular Formula:C21H15F4N5O2S
  • Molecular Weight:477.442
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Product Details

Purity:99%

Reputable factory supply Apalutamide 956104-40-8 in stock with high standard

  • Molecular Formula:C21H15F4N5O2S
  • Molecular Weight:477.442
  • PKA:13.83±0.46(Predicted) 
  • PSA:121.42000 
  • Density:1.59±0.1 g/cm3(Predicted) 
  • LogP:4.05248 

956104-40-8 Relevant articles

Process for the preparation of 4-[7-(6-Cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7- diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide and its polymorphs

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, (2021/06/22)

The present application relates a proces...

PROCESS FOR THE PREPARATION OF APALUTAMIDE

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Paragraph 11-12, (2021/02/26)

Aspect of the present application relate...

Alluzole intermediate and method for preparing

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, (2021/09/21)

The invention relates to an intermediate...

Method for preparing

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Paragraph 0100-0104, (2021/08/25)

The invention relates to a method for pr...

956104-40-8 Process route

2-fluoro-N-methyl-4-amino-benzamide
915087-25-1

2-fluoro-N-methyl-4-amino-benzamide

ARN-509
956104-40-8

ARN-509

Conditions
Conditions Yield
Multi-step reaction with 2 steps
1.1: acetic acid / 16 h / 80 °C
2.1: N,N-dimethyl acetamide / 16 h / 60 °C
2.2: 1 h / Reflux
With acetic acid; In N,N-dimethyl acetamide;
Multi-step reaction with 2 steps
1.1: acetic acid / 24 h / 80 °C
2.1: N,N-dimethyl-formamide / 20 h / 80 °C / Microwave irradiation
2.2: 2 h
With acetic acid; In N,N-dimethyl-formamide;
Multi-step reaction with 2 steps
1.1: acetic acid / 16 h / 80 °C / Sealed tube
2.1: N,N-dimethyl acetamide / 16 h / 60 °C / Inert atmosphere
2.2: 2 h / Reflux; Inert atmosphere
With acetic acid; In N,N-dimethyl acetamide;
Multi-step reaction with 2 steps
1.1: triethylamine / dichloromethane / 20 h / 20 °C
1.2: 4 h / Reflux
1.3: 16 h / 20 °C
2.1: N,N-dimethyl-formamide / 16 h / 80 °C / Sealed tube
With triethylamine; In dichloromethane; N,N-dimethyl-formamide;
Multi-step reaction with 3 steps
1.1: triethylamine / dichloromethane / 20 h / 20 °C
1.2: 4 h / Reflux
1.3: 16 h / 20 °C
2.1: thionyl chloride / 16 h / 0 - 40 °C
3.1: pyridine / 4.75 h / 60 °C
With pyridine; thionyl chloride; triethylamine; In dichloromethane;
Multi-step reaction with 3 steps
1.1: triethylamine / dichloromethane / 20 h / 20 °C
1.2: 4 h / Reflux
1.3: 16 h / 20 °C
2.1: dicyclohexyl-carbodiimide / dichloromethane; ethyl acetate / 2 h / -15 - 0 °C
3.1: pyridine / 112 h / 20 - 60 °C / Sealed tube
With pyridine; triethylamine; dicyclohexyl-carbodiimide; In dichloromethane; ethyl acetate;
Multi-step reaction with 2 steps
1.1: acetic acid / tetrahydrofuran / 26.17 h / 25 - 85 °C
2.1: Isopropyl acetate; N,N-dimethyl-formamide / 65 - 70 °C
2.2: 3 h / 25 - 85 °C
With acetic acid; In tetrahydrofuran; Isopropyl acetate; N,N-dimethyl-formamide;
4-bromo-2-fluoro-N-methylbenzanamide
749927-69-3

4-bromo-2-fluoro-N-methylbenzanamide

ARN-509
956104-40-8

ARN-509

Conditions
Conditions Yield
Multi-step reaction with 3 steps
1.1: potassium carbonate / N,N-dimethyl-formamide; water / 18 h / 100 °C
2.1: potassium carbonate / N,N-dimethyl-formamide / 0.17 h / 50 °C
2.2: 10 h / 0 - 20 °C
3.1: dimethyl sulfoxide / 1 h / 85 °C / Inert atmosphere
With potassium carbonate; In water; dimethyl sulfoxide; N,N-dimethyl-formamide;
Multi-step reaction with 3 steps
1.1: potassium carbonate / N,N-dimethyl-formamide; water / 18 h / 100 °C
2.1: potassium carbonate / N,N-dimethyl-formamide / 0.17 h / 50 °C
2.2: 5 h / 50 °C
3.1: dimethyl sulfoxide / 85 °C / Inert atmosphere
With potassium carbonate; In water; dimethyl sulfoxide; N,N-dimethyl-formamide;
Multi-step reaction with 3 steps
1.1: potassium carbonate / N,N-dimethyl-formamide; water / 18 h / 100 °C
2.1: dmap / dichloromethane / 0.17 h
2.2: 24 h / 0 - 20 °C
3.1: dimethyl sulfoxide / 8 h / 85 °C / Inert atmosphere
With dmap; potassium carbonate; In dichloromethane; water; dimethyl sulfoxide; N,N-dimethyl-formamide;
Multi-step reaction with 3 steps
1.1: potassium carbonate / N,N-dimethyl-formamide; water / 18 h / 100 °C
2.1: dmap / dichloromethane / 0.17 h
2.2: 24 h / 0 - 20 °C
3.1: dimethyl sulfoxide / 85 °C / Inert atmosphere
With dmap; potassium carbonate; In dichloromethane; water; dimethyl sulfoxide; N,N-dimethyl-formamide;
Multi-step reaction with 3 steps
1: potassium carbonate / N,N-dimethyl-formamide; water / 18 h / 100 °C
2: potassium carbonate / N,N-dimethyl-formamide; water / 1 h / 30 - 40 °C
3: dimethyl sulfoxide / 8 h / 80 °C
With potassium carbonate; In water; dimethyl sulfoxide; N,N-dimethyl-formamide;
Multi-step reaction with 3 steps
1: potassium carbonate / N,N-dimethyl-formamide; water / 18 h / 100 °C
2: potassium carbonate / N,N-dimethyl-formamide; water / 5 h / 30 - 50 °C
3: dimethyl sulfoxide / 5 h / 85 °C
With potassium carbonate; In water; dimethyl sulfoxide; N,N-dimethyl-formamide;
Multi-step reaction with 3 steps
1: 2-acetylcyclohexanone; potassium carbonate; copper(l) chloride / N,N-dimethyl acetamide; water / 8 h / 95 - 105 °C / Inert atmosphere
2: potassium carbonate / N,N-dimethyl acetamide / 1 h / 20 - 45 °C / Inert atmosphere
3: acetonitrile / 40 h / 85 °C
With 2-acetylcyclohexanone; potassium carbonate; copper(l) chloride; In N,N-dimethyl acetamide; water; acetonitrile;
Multi-step reaction with 4 steps
1: caesium carbonate; copper(l) iodide / N,N-dimethyl acetamide / 90 - 95 °C / Inert atmosphere
2: thionyl chloride / 40 - 45 °C
3: N-ethyl-N,N-diisopropylamine / methanol / Reflux
4: potassium carbonate; copper(l) iodide / N,N-dimethyl-formamide / 100 - 110 °C / Inert atmosphere
With copper(l) iodide; thionyl chloride; potassium carbonate; caesium carbonate; N-ethyl-N,N-diisopropylamine; In methanol; N,N-dimethyl acetamide; N,N-dimethyl-formamide;
Multi-step reaction with 2 steps
1: copper(l) iodide; potassium carbonate; triethylamine; 2-acetylcyclohexanone / water; N,N-dimethyl-formamide / 60 h / 95 - 100 °C
2: N,N-dimethyl-formamide / 16 h / 80 °C / Sealed tube
With copper(l) iodide; 2-acetylcyclohexanone; potassium carbonate; triethylamine; In water; N,N-dimethyl-formamide;
Multi-step reaction with 3 steps
1: copper(l) iodide; potassium carbonate; triethylamine; 2-acetylcyclohexanone / water; N,N-dimethyl-formamide / 60 h / 95 - 100 °C
2: thionyl chloride / 16 h / 0 - 40 °C
3: pyridine / 4.75 h / 60 °C
With pyridine; copper(l) iodide; thionyl chloride; 2-acetylcyclohexanone; potassium carbonate; triethylamine; In water; N,N-dimethyl-formamide;
Multi-step reaction with 3 steps
1: copper(l) iodide; potassium carbonate; triethylamine; 2-acetylcyclohexanone / water; N,N-dimethyl-formamide / 60 h / 95 - 100 °C
2: dicyclohexyl-carbodiimide / dichloromethane; ethyl acetate / 2 h / -15 - 0 °C
3: pyridine / 112 h / 20 - 60 °C / Sealed tube
With pyridine; copper(l) iodide; 2-acetylcyclohexanone; potassium carbonate; triethylamine; dicyclohexyl-carbodiimide; In dichloromethane; water; ethyl acetate; N,N-dimethyl-formamide;
Multi-step reaction with 3 steps
1.1: potassium carbonate; copper(l) chloride / N,N-dimethyl-formamide / 10.5 h / 20 - 110 °C / Inert atmosphere
2.1: potassium carbonate / N,N-dimethyl-formamide / 0.5 h / 20 °C
2.2: 2 h / 40 °C
3.1: N,N-dimethyl-formamide / 8 h / 85 °C / Inert atmosphere
With potassium carbonate; copper(l) chloride; In N,N-dimethyl-formamide;
Multi-step reaction with 3 steps
1: potassium carbonate; copper(l) chloride / N,N-dimethyl-formamide / 10.5 h / 20 - 110 °C / Inert atmosphere
2: sulfuric acid / 20 h / Reflux
3: N,N-dimethyl-formamide / 8 h / 85 °C / Inert atmosphere
With sulfuric acid; potassium carbonate; copper(l) chloride; In N,N-dimethyl-formamide;
Multi-step reaction with 3 steps
1: potassium carbonate; copper(l) chloride / N,N-dimethyl-formamide / 10.5 h / 20 - 110 °C / Inert atmosphere
2: acetyl chloride / 10 h / Reflux
3: dimethylsulfoxide-d6 / 12 h / 85 °C / Inert atmosphere
With potassium carbonate; acetyl chloride; copper(l) chloride; In dimethylsulfoxide-d6; N,N-dimethyl-formamide;
Multi-step reaction with 3 steps
1: potassium carbonate; copper(l) chloride / N,N-dimethyl-formamide / 10.5 h / 20 - 110 °C / Inert atmosphere
2: acetyl chloride / 10 h / Reflux
3: dimethyl sulfoxide; Isopropyl acetate / 12 h / 85 °C / Inert atmosphere
With potassium carbonate; acetyl chloride; copper(l) chloride; In Isopropyl acetate; dimethyl sulfoxide; N,N-dimethyl-formamide;

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