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761440-16-8

  • Product Name:4-Pyrimidinamine, 2,5-dichloro-N-[2-[(1-methylethyl)sulfonyl]phenyl]-
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Product Details

Purity:99%

Pharmaceutical grade 4-Pyrimidinamine, 2,5-dichloro-N-[2-[(1-methylethyl)sulfonyl]phenyl]- 761440-16-8 Good Manufacturer

  • Molecular Formula:C13H13Cl2N3O2S
  • Molecular Weight:346.237
  • Melting Point:149.0 to 153.0 °C 
  • Boiling Point:538℃ 
  • PKA:-0.03±0.10(Predicted) 
  • Flash Point:279℃ 
  • PSA：80.33000 
  • Density:1.436 
  • LogP:4.86290 

2,5-dichloro-N-(2-(isopropylsulfonyl)phenyl)pyrimidin-4-amine(Cas 761440-16-8) Usage

Uses

2,5-Dichloro-N-[2-(isopropylsulfonyl)phenyl]pyrimidin-4-amine is used as a reagent in the synthesis of potent and selective anaplastic lymphoma kinase (ALK-5) inhibitors, used as an anti-tumor treatment.

InChI:InChI=1S/C13H13Cl2N3O2S/c1-8(2)21(19,20)11-6-4-3-5-10(11)17-12-9(14)7-16-13(15)18-12/h3-8H,1-2H3,(H,16,17,18)

761440-16-8 Relevant articles

Discovery of novel mutant-combating ALK and ROS1 dual inhibitors bearing imidazolidin-2-one moiety with reasonable PK properties

Lei, Hongrui,Jiang, Nan,Miao, Xiuqi,Xing, Lingyun,Guo, Ming,Liu, Yang,Xu, Haowen,Gong, Ping,Zuo, Daiying,Zhai, Xin

, p. 297 - 309 (2019)

Aiming to identify novel potent ALK and ...

Small molecule inhibitors of leucine-rich repetitive kinase 2 and their applications

-

Paragraph 0078-0082, (2022/01/07)

The present invention provides a small m...

POTENT AND SELECTIVE DEGRADERS OF ALK

-

Paragraph 00212-00213, (2021/09/04)

Disclosed are bispecific compounds (degr...

CDK inhibitor based on organic arsine as well as preparation method and application of CDK inhibitor

-

Paragraph 0412-0414; 0424-0426, (2021/03/31)

The invention provides a CDK inhibitor b...

CHEMICAL PROCESS FOR PREPARING PYRIMIDINE DERIVATIVES AND INTERMEDIATES THEREOF

-

Paragraph 0174-0175; 0177, (2021/05/21)

PROBLEM TO BE SOLVED: To provide a proce...

761440-16-8 Process route

1-amino-2-(isopropylsulphonyl)benzene
76697-50-2

1-amino-2-(isopropylsulphonyl)benzene

2,4,5-trichloropyrimidine
5750-76-5

2,4,5-trichloropyrimidine

2-chloro-N-(2-(isopropylsulfonyl)phenyl)-5-methyl-pyrimidin-4-amine
761440-16-8

2-chloro-N-(2-(isopropylsulfonyl)phenyl)-5-methyl-pyrimidin-4-amine

Conditions
Conditions Yield
With potassium tert-butylate; zinc diacetate; In 1-methyl-pyrrolidin-2-one; at 118 - 122 ℃; for 10h; Reagent/catalyst; Temperature; Solvent;
92.1%
1-amino-2-(isopropylsulphonyl)benzene; With sodium hydride; In dimethyl sulfoxide; N,N-dimethyl-formamide; at 0 ℃; for 0.5h; Inert atmosphere;
2,4,5-trichloropyrimidine; In dimethyl sulfoxide; N,N-dimethyl-formamide; at 0 - 20 ℃; Inert atmosphere;
90.6%
2,4,5-trichloropyrimidine; With sodium hydride; In N,N-dimethyl-formamide; mineral oil; at 0 ℃; for 0.5h;
1-amino-2-(isopropylsulphonyl)benzene; In N,N-dimethyl-formamide; mineral oil; at 0 - 20 ℃; for 2h;
72%
With palladium diacetate; caesium carbonate; triphenylphosphine; In toluene; for 4h; Inert atmosphere; Reflux;
65.6%
1-amino-2-(isopropylsulphonyl)benzene; With sodium hydride; In N,N-dimethyl-formamide; mineral oil; at 0 ℃; for 1h; Ionic liquid;
2,4,5-trichloropyrimidine; In N,N-dimethyl-formamide; mineral oil; at 20 ℃;
63%
1-amino-2-(isopropylsulphonyl)benzene; With sodium hydride; In dimethyl sulfoxide; N,N-dimethyl-formamide; at 0 ℃;
2,4,5-trichloropyrimidine; In dimethyl sulfoxide; N,N-dimethyl-formamide; at 0 - 20 ℃;
60%
1-amino-2-(isopropylsulphonyl)benzene; With sodium hydride; In dimethyl sulfoxide; N,N-dimethyl-formamide; at 0 ℃; for 0.75h; Inert atmosphere;
2,4,5-trichloropyrimidine; In dimethyl sulfoxide; N,N-dimethyl-formamide; at 0 - 20 ℃; for 2.75h;
60.6%
1-amino-2-(isopropylsulphonyl)benzene; With sodium hydride; In N,N-dimethyl-formamide; at 0 ℃; for 0.5h;
2,4,5-trichloropyrimidine; In N,N-dimethyl-formamide; at 0 - 20 ℃; regioselective reaction;
59%
With sodium hydride; In dimethyl sulfoxide; N,N-dimethyl-formamide; mineral oil; at 20 ℃; for 16h; Concentration; Solvent; Cooling with ice;
52%
1-amino-2-(isopropylsulphonyl)benzene; With sodium hydride; In N,N-dimethyl-formamide; mineral oil; at 0 ℃; for 0.5h;
2,4,5-trichloropyrimidine; In N,N-dimethyl-formamide; mineral oil; at 20 ℃;
48%
With sodium hydride; In N,N-dimethyl-formamide; mineral oil; at 25 ℃; for 12h; Temperature; Solvent;
46%
With sodium hydride; In N,N-dimethyl-formamide; mineral oil; at 25 ℃; for 12h;
46%
1-amino-2-(isopropylsulphonyl)benzene; With sodium hydride; In dimethyl sulfoxide; N,N-dimethyl-formamide; at 0 ℃; for 0.5h;
2,4,5-trichloropyrimidine; In dimethyl sulfoxide; N,N-dimethyl-formamide; at 0 - 20 ℃; for 15h;
40.6%
1-amino-2-(isopropylsulphonyl)benzene; With sodium hydride; In N,N-dimethyl-formamide; at 0 ℃; for 0.5h;
2,4,5-trichloropyrimidine; In N,N-dimethyl-formamide; at 20 ℃; for 12h;
40%
1-amino-2-(isopropylsulphonyl)benzene; With sodium hydride; In N,N-dimethyl-formamide; mineral oil; for 0.5h; Cooling with ice;
2,4,5-trichloropyrimidine; In N,N-dimethyl-formamide; mineral oil; for 10h; Cooling with ice;
40%
1-amino-2-(isopropylsulphonyl)benzene; With sodium hydride; In N,N-dimethyl-formamide; mineral oil; for 0.5h; Cooling with ice;
2,4,5-trichloropyrimidine; In N,N-dimethyl-formamide; for 10h; Cooling with ice;
40%
1-amino-2-(isopropylsulphonyl)benzene; With sodium hydride; In N,N-dimethyl-formamide; for 0.5h; Cooling with ice;
2,4,5-trichloropyrimidine; In N,N-dimethyl-formamide; at 20 ℃; Cooling with ice;
40%
1-amino-2-(isopropylsulphonyl)benzene; With sodium hydride; In N,N-dimethyl-formamide; at 0 ℃; for 0.666667h;
2,4,5-trichloropyrimidine; In N,N-dimethyl-formamide; at 0 - 20 ℃;
35%
1-amino-2-(isopropylsulphonyl)benzene; With sodium hydride; In N,N-dimethyl-formamide; at 0 ℃; for 0.25h;
2,4,5-trichloropyrimidine; In N,N-dimethyl-formamide; at 20 ℃;
33%
1-amino-2-(isopropylsulphonyl)benzene; With sodium hydride; In N,N-dimethyl-formamide; for 0.25h; Cooling;
2,4,5-trichloropyrimidine; In N,N-dimethyl-formamide; at 20 ℃; for 16h;
32.69%
1-amino-2-(isopropylsulphonyl)benzene; With sodium hydride; In N,N-dimethyl-formamide; at 0 ℃; for 0.25h;
2,4,5-trichloropyrimidine; In N,N-dimethyl-formamide; at 20 ℃;
32%
1-amino-2-(isopropylsulphonyl)benzene; With sodium hydride; In N,N-dimethyl-formamide; at 0 - 5 ℃; for 0.25h;
2,4,5-trichloropyrimidine; In N,N-dimethyl-formamide; at 0 - 5 ℃;
32.7%
1-amino-2-(isopropylsulphonyl)benzene; With sodium hydride; In N,N-dimethyl-formamide; mineral oil; at 0 ℃; for 0.333333h;
2,4,5-trichloropyrimidine; In N,N-dimethyl-formamide; mineral oil; at 0 - 20 ℃; for 2.5h;
20%
With N-ethyl-N,N-diisopropylamine; In isopropyl alcohol; for 2h; Reflux;
17%
1-amino-2-(isopropylsulphonyl)benzene; With sodium hydride; In N,N-dimethyl-formamide; mineral oil; at 0 ℃; for 0.5h;
2,4,5-trichloropyrimidine; In N,N-dimethyl-formamide; mineral oil; at 0 - 20 ℃; for 12h;
 
With sodium hydride; In N,N-dimethyl-formamide;
 
1-amino-2-(isopropylsulphonyl)benzene; With sodium hydride; In N,N-dimethyl-formamide; mineral oil; at 0 ℃; for 4h; Inert atmosphere;
2,4,5-trichloropyrimidine; In N,N-dimethyl-formamide; mineral oil; at 0 ℃; for 4h; Inert atmosphere;
 
With potassium carbonate; In N,N-dimethyl-formamide; at 75 ℃;
 
1-amino-2-(isopropylsulphonyl)benzene; With sodium hydride; In N,N-dimethyl acetamide; at 0 ℃; for 1h;
2,4,5-trichloropyrimidine; In N,N-dimethyl acetamide; at 20 - 25 ℃; for 2h; Reagent/catalyst; Time; Temperature;
9.1 g
1-amino-2-(isopropylsulphonyl)benzene; With sodium hydride; In N,N-dimethyl-formamide; at 20 ℃; for 0.5h; Cooling with ice;
2,4,5-trichloropyrimidine; In N,N-dimethyl-formamide; at 20 ℃; for 16h;
1.7 g
With 1,8-diazabicyclo[5.4.0]undec-7-ene; at 80 ℃; for 7.5h;
 
With sodium hydride; In N,N-dimethyl-formamide; at 20 ℃;
0.5 g
With 1,8-diazabicyclo[5.4.0]undec-7-ene; In tetrahydrofuran; at 80 ℃; Solvent; Temperature; Reagent/catalyst; Inert atmosphere;
0.88 g
With sodium hydride; In dimethyl sulfoxide;
 
1-amino-2-(isopropylsulphonyl)benzene; With sodium hydride; In N,N-dimethyl-formamide; at -10 ℃; for 0.5h;
2,4,5-trichloropyrimidine; In N,N-dimethyl-formamide; at 20 ℃; for 6h;
 
With 1,8-diazabicyclo[5.4.0]undec-7-ene; at 80 ℃; for 7.5h;
 
With 1,8-diazabicyclo[5.4.0]undec-7-ene; at 80 ℃; for 7.5h; Large scale;
1.07 kg
1-amino-2-(isopropylsulphonyl)benzene; With sodium hydride; In dimethyl sulfoxide; N,N-dimethyl-formamide; at 0 ℃; for 0.5h;
2,4,5-trichloropyrimidine;
 
1-amino-2-(isopropylsulphonyl)benzene; With sodium hydride; In N,N-dimethyl-formamide; at 0 ℃; for 0.5h;
2,4,5-trichloropyrimidine; In N,N-dimethyl-formamide; at 20 ℃; for 2h;
2.7 g
1-amino-2-(isopropylsulphonyl)benzene; With sodium hydride; In N,N-dimethyl-formamide; at 0 ℃; for 0.5h;
2,4,5-trichloropyrimidine; In N,N-dimethyl-formamide; at 20 ℃; for 2h;
2.7 g
With 1,8-diazabicyclo[5.4.0]undec-7-ene; at 80 ℃; for 7.5h; Large scale;
 
2,6-dichloro-5-methylpyrimidine
1780-31-0

2,6-dichloro-5-methylpyrimidine

1-amino-2-(isopropylsulphonyl)benzene
76697-50-2

1-amino-2-(isopropylsulphonyl)benzene

2-chloro-N-(2-(isopropylsulfonyl)phenyl)-5-methyl-pyrimidin-4-amine
761440-16-8

2-chloro-N-(2-(isopropylsulfonyl)phenyl)-5-methyl-pyrimidin-4-amine

Conditions
Conditions Yield
1-amino-2-(isopropylsulphonyl)benzene; With sodium hydride; In N,N-dimethyl-formamide; at 0 ℃; for 0.5h;
2,6-dichloro-5-methylpyrimidine; In N,N-dimethyl-formamide; at 20 ℃;
59%

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