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16013-85-7 Usage

Chemical Properties

yellow crystalline powder or chunks

Uses

2,6-Dichloro-3-nitropyridine was used:in the synthesis of pyridyldifluoroacetatesas starting reagent in the preparation of bicyclooxacalixhetarene

General Description

2,6-Dichloro-3-nitropyridine undergoes macrocyclic condensation reaction with resorcinol derivatives to yield chiral tetraoxacalix[2]arene[2]pyridines.

Check Digit Verification of cas no

The CAS Registry Mumber 16013-85-7 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 1,6,0,1 and 3 respectively; the second part has 2 digits, 8 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 16013-85:
(7*1)+(6*6)+(5*0)+(4*1)+(3*3)+(2*8)+(1*5)=77
77 % 10 = 7
So 16013-85-7 is a valid CAS Registry Number.
InChI:InChI=1/C5H2Cl2N2O2/c6-4-2-1-3(9(10)11)5(7)8-4/h1-2H

16013-85-7 Well-known Company Product Price

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  • (Code)Product description
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  • Detail
  • Alfa Aesar

  • (B21255)  2,6-Dichloro-3-nitropyridine, 97%   

  • 16013-85-7

  • 10g

  • 637.0CNY

  • Detail
  • Alfa Aesar

  • (B21255)  2,6-Dichloro-3-nitropyridine, 97%   

  • 16013-85-7

  • 50g

  • 2322.0CNY

  • Detail
  • Alfa Aesar

  • (B21255)  2,6-Dichloro-3-nitropyridine, 97%   

  • 16013-85-7

  • 250g

  • 8196.0CNY

  • Detail
  • Aldrich

  • (193585)  2,6-Dichloro-3-nitropyridine  technical grade, 92%

  • 16013-85-7

  • 193585-10G

  • 727.74CNY

  • Detail

16013-85-7SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 10, 2017

Revision Date: Aug 10, 2017

1.Identification

1.1 GHS Product identifier

Product name 2,6-Dichloro-3-nitropyridine

1.2 Other means of identification

Product number -
Other names 3-Nitro-2,6-dichloropyridine

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:16013-85-7 SDS

16013-85-7Synthetic route

2,6-dihydroxy-3-nitropyridine
16013-84-6

2,6-dihydroxy-3-nitropyridine

2,6-dicholoro-3-nitropyridine
16013-85-7

2,6-dicholoro-3-nitropyridine

Conditions
ConditionsYield
With bis(trichloromethyl) carbonate In N,N-dimethyl-formamide at 80 - 85℃; for 6h; Solvent; Temperature; Reagent/catalyst;92.9%
4-ethoxycarbonylpiperazine
120-43-4

4-ethoxycarbonylpiperazine

A

2,6-dicholoro-3-nitropyridine
16013-85-7

2,6-dicholoro-3-nitropyridine

B

2-chloro-6-(4-ethoxycarbonyl-1-piperazinyl)-3-nitropyridine
92741-37-2

2-chloro-6-(4-ethoxycarbonyl-1-piperazinyl)-3-nitropyridine

C

4-(6-chloro-3-nitro-2-pyridinyl)-1-piperazinecarboxylic acid,ethyl ester
75167-21-4

4-(6-chloro-3-nitro-2-pyridinyl)-1-piperazinecarboxylic acid,ethyl ester

D

2,6-bis(4-ethoxycarbonyl-1-piperazinyl)-3-nitropyridine
92741-38-3

2,6-bis(4-ethoxycarbonyl-1-piperazinyl)-3-nitropyridine

Conditions
ConditionsYield
With hydrogenchloride; triethylamine In chloroform at -5 - 0℃; for 2h;A 1%
B 8%
C 91.3%
D 3.1%
With hydrogenchloride; triethylamine In chloroform at -5 - 0℃; for 2h;A 1%
B 8%
C 91.3%
D 3.1%
2,6-dichloropyridine
2402-78-0

2,6-dichloropyridine

2,6-dicholoro-3-nitropyridine
16013-85-7

2,6-dicholoro-3-nitropyridine

Conditions
ConditionsYield
With sulfuric acid; nitric acid at 120℃; for 5h; Cooling with ice;81%
With sulfuric acid; potassium nitrate at 20 - 120℃; for 10.5h;80%
With sulfuric acid; nitric acid In water at 20 - 105℃; for 5h;75.38%
(2,6-dichloropyridin-3-yl)boronic acid
148493-34-9

(2,6-dichloropyridin-3-yl)boronic acid

2,6-dicholoro-3-nitropyridine
16013-85-7

2,6-dicholoro-3-nitropyridine

Conditions
ConditionsYield
With N–nitrosuccinimide; tris(2,2-bipyridine)ruthenium(II) hexafluorophosphate In acetonitrile at 20℃; for 19h; Inert atmosphere; Irradiation;65%
K2 CO3 powder

K2 CO3 powder

2,6-dicholoro-3-nitropyridine
16013-85-7

2,6-dicholoro-3-nitropyridine

A

6-chloro-2-methoxy-3-nitropyridine
40851-91-0

6-chloro-2-methoxy-3-nitropyridine

B

2-chloro-6-methoxy-3-nitropyridine
38533-61-8

2-chloro-6-methoxy-3-nitropyridine

Conditions
ConditionsYield
In methanol; ethyl acetateA n/a
B 100%
In methanol; ethyl acetateA n/a
B 100%
4-methylpiperidin
626-58-4

4-methylpiperidin

2,6-dicholoro-3-nitropyridine
16013-85-7

2,6-dicholoro-3-nitropyridine

6'-chloro-4-methyl-3'-nitro-3,4,5,6-tetrahydro-2H-[1,2']bipyridinyl
885704-86-9

6'-chloro-4-methyl-3'-nitro-3,4,5,6-tetrahydro-2H-[1,2']bipyridinyl

Conditions
ConditionsYield
With potassium carbonate In toluene at 20℃; for 6.5h; Product distribution / selectivity;100%
In ethanol at 20℃; for 15h; Product distribution / selectivity;45%
In tetrahydrofuran
2,6-dicholoro-3-nitropyridine
16013-85-7

2,6-dicholoro-3-nitropyridine

N,N-bis(p-methoxybenzyl)amine
17061-62-0

N,N-bis(p-methoxybenzyl)amine

6-chloro-N,N-bis(4-methoxybenzyl)-3-nitropyridin-2-amine
928831-85-0

6-chloro-N,N-bis(4-methoxybenzyl)-3-nitropyridin-2-amine

Conditions
ConditionsYield
Stage #1: 2,6-dicholoro-3-nitropyridine; N,N-bis(p-methoxybenzyl)amine With triethylamine In chloroform at 0 - 20℃;
Stage #2: In dichloromethane at 20℃; for 48h;
100%
3-methyl-3-nitro-butylamine hydrochloride
5336-19-6

3-methyl-3-nitro-butylamine hydrochloride

2,6-dicholoro-3-nitropyridine
16013-85-7

2,6-dicholoro-3-nitropyridine

(6-chloro-3-nitro-pyridin-2-yl)-(3-methyl-3-nitro-butyl)-amine
935847-72-6

(6-chloro-3-nitro-pyridin-2-yl)-(3-methyl-3-nitro-butyl)-amine

Conditions
ConditionsYield
With triethylamine In dichloromethane at 20℃; for 20h;100%
2,6-dicholoro-3-nitropyridine
16013-85-7

2,6-dicholoro-3-nitropyridine

ethyl β-alaninate hydrochloride
4244-84-2

ethyl β-alaninate hydrochloride

ethyl 3-((6-chloro-3-nitropyridin-2-yl)amino)propanoate
433226-12-1

ethyl 3-((6-chloro-3-nitropyridin-2-yl)amino)propanoate

Conditions
ConditionsYield
With N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 20℃;100%
2,6-dicholoro-3-nitropyridine
16013-85-7

2,6-dicholoro-3-nitropyridine

isopropyl alcohol
67-63-0

isopropyl alcohol

6-chloro-3-nitro-2-(propan-2-yloxy)pyridine
186413-77-4

6-chloro-3-nitro-2-(propan-2-yloxy)pyridine

Conditions
ConditionsYield
With sodium hydride In toluene; mineral oil at 5 - 20℃;100%
Stage #1: 2,6-dicholoro-3-nitropyridine; isopropyl alcohol In toluene at 0℃; for 0.25h;
Stage #2: With sodium hydride In toluene at 0 - 20℃; for 16.25h; Inert atmosphere;
98%
With sodium hydride In toluene at 0 - 20℃; for 16.5h; Inert atmosphere; regioselective reaction;93%
2,6-dicholoro-3-nitropyridine
16013-85-7

2,6-dicholoro-3-nitropyridine

(R)-1-phenylpropylamine
3789-59-1

(R)-1-phenylpropylamine

6-chloro-3-nitro-N-[(1S)-1-phenylpropyl]pyridin-2-amine

6-chloro-3-nitro-N-[(1S)-1-phenylpropyl]pyridin-2-amine

Conditions
ConditionsYield
Stage #1: 2,6-dicholoro-3-nitropyridine; (R)-1-phenylpropylamine In dichloromethane at -70 - 70℃; for 0.0833333h;
Stage #2: With N-ethyl-N,N-diisopropylamine In dichloromethane at 20 - 70℃; for 18h;
99.7%
2,6-dicholoro-3-nitropyridine
16013-85-7

2,6-dicholoro-3-nitropyridine

ethylamine
75-04-7

ethylamine

6-chloro-N-ethyl-3-nitropyridin-2-amine
33742-69-7

6-chloro-N-ethyl-3-nitropyridin-2-amine

Conditions
ConditionsYield
With triethylamine In tert-butyl methyl ether at -5 - 20℃; Inert atmosphere;99%
Stage #1: 2,6-dicholoro-3-nitropyridine With sodium carbonate In ethanol for 0.5h; Cooling with ice;
Stage #2: ethylamine In ethanol for 0.5h;
77%
In toluene at 0 - 20℃; for 3h; Inert atmosphere;38%
2,6-dicholoro-3-nitropyridine
16013-85-7

2,6-dicholoro-3-nitropyridine

2,6-dibromo-3-nitropyridine
55304-80-8

2,6-dibromo-3-nitropyridine

Conditions
ConditionsYield
With hydrogen bromide; acetic acid at 80℃; for 3h;99%
With hydrogen bromide; acetic acid In water at 80℃; for 18h;94%
With bromine; acetic acid at 50℃;88%
With hydrogen bromide; acetic acid In water at 50℃;87%
Stage #1: 2,6-dicholoro-3-nitropyridine With hydrogen bromide; acetic acid at 80℃; for 6h;
Stage #2: With sodium hydroxide In water at 0℃;
2,6-dicholoro-3-nitropyridine
16013-85-7

2,6-dicholoro-3-nitropyridine

tert-butylamine
75-64-9

tert-butylamine

N-tert-butyl-6-chloro-3-nitropyridin-2-amine
1094323-29-1

N-tert-butyl-6-chloro-3-nitropyridin-2-amine

Conditions
ConditionsYield
In toluene at 0 - 20℃; for 14.5h;99%
In toluene at 0 - 20℃; for 16h;79%
In tetrahydrofuran at 20℃;46%
2,6-dicholoro-3-nitropyridine
16013-85-7

2,6-dicholoro-3-nitropyridine

N-butylamine
109-73-9

N-butylamine

6-chloro-N-butyl-3-nitropyridin-2-amine
1094235-54-7

6-chloro-N-butyl-3-nitropyridin-2-amine

Conditions
ConditionsYield
With triethylamine In tert-butyl methyl ether at -5 - 20℃; Inert atmosphere;98.4%
Stage #1: N-butylamine With sodium hydride In toluene at 0℃; Inert atmosphere;
Stage #2: 2,6-dicholoro-3-nitropyridine In toluene at 20℃; Inert atmosphere;
Stage #1: 2,6-dicholoro-3-nitropyridine With potassium carbonate In ethanol Cooling with ice;
Stage #2: N-butylamine In ethanol
5.5 g
2,6-dicholoro-3-nitropyridine
16013-85-7

2,6-dicholoro-3-nitropyridine

3-amino-5-cyclopropyl-1H-pyrazole
175137-46-9

3-amino-5-cyclopropyl-1H-pyrazole

6-chloro-N-(5-cyclopropyl-1H-pyrazol-3-yl)-3-nitropyridin-2-amine
685867-14-5

6-chloro-N-(5-cyclopropyl-1H-pyrazol-3-yl)-3-nitropyridin-2-amine

Conditions
ConditionsYield
With N-ethyl-N,N-diisopropylamine In ethanol at 25℃; for 24h;98%
With N-ethyl-N,N-diisopropylamine In ethanol at 0 - 25℃; for 24h;98%
With N-ethyl-N,N-diisopropylamine In acetonitrile at 20℃; for 24h;69%
With N-ethyl-N,N-diisopropylamine In acetonitrile at 20℃; for 2h;
2,6-dicholoro-3-nitropyridine
16013-85-7

2,6-dicholoro-3-nitropyridine

ethyl 2-sulfanylacetate
623-51-8

ethyl 2-sulfanylacetate

diethyl 2,2'-[(3-nitropyridine-2,6-diyl)bissulfanediyl]diacetate
1378233-77-2

diethyl 2,2'-[(3-nitropyridine-2,6-diyl)bissulfanediyl]diacetate

Conditions
ConditionsYield
Stage #1: ethyl 2-sulfanylacetate With sodium hydride In tetrahydrofuran for 0.5h; Inert atmosphere;
Stage #2: 2,6-dicholoro-3-nitropyridine In tetrahydrofuran for 0.25h; Inert atmosphere;
97%
2,6-dicholoro-3-nitropyridine
16013-85-7

2,6-dicholoro-3-nitropyridine

2-methyl-propan-1-ol
78-83-1

2-methyl-propan-1-ol

6-chloro-2-isobutoxy-3-nitropyridine

6-chloro-2-isobutoxy-3-nitropyridine

Conditions
ConditionsYield
With sodium hydride In toluene; mineral oil for 4.5h; Inert atmosphere; regioselective reaction;96%
2,6-dicholoro-3-nitropyridine
16013-85-7

2,6-dicholoro-3-nitropyridine

2,5-dichloro-benzylamine
10541-69-2

2,5-dichloro-benzylamine

6-chloro-N-[(2,5-dichlorophenyl)methyl]-3-nitropyridin-2-amine

6-chloro-N-[(2,5-dichlorophenyl)methyl]-3-nitropyridin-2-amine

Conditions
ConditionsYield
With sodium hydride In toluene; mineral oil at 0 - 20℃; for 18h;96%
pyrrolidine
123-75-1

pyrrolidine

2,6-dicholoro-3-nitropyridine
16013-85-7

2,6-dicholoro-3-nitropyridine

6-chloro-3-nitro-2-(pyrrolidin-1-yl)pyridine
92741-40-7

6-chloro-3-nitro-2-(pyrrolidin-1-yl)pyridine

Conditions
ConditionsYield
In dichloromethane at 0 - 20℃; for 17h;95%
With hydrogenchloride; triethylamine In chloroform at -5 - 0℃; for 2h;88.4%
With triethylamine In acetonitrile at 0 - 20℃; for 3h;85%
In dichloromethane Cooling with ice;79%
2,6-dicholoro-3-nitropyridine
16013-85-7

2,6-dicholoro-3-nitropyridine

3-amino-2,6-dichloropyridine
62476-56-6

3-amino-2,6-dichloropyridine

Conditions
ConditionsYield
With iron; acetic acid at 20℃; for 6h;95%
With hydrogenchloride; acetic acid; tin(ll) chloride at 20℃; for 3h;94.8%
With hydrogen In tetrahydrofuran at 37℃; under 2250.23 Torr; for 16h; chemoselective reaction;92%
5-propan-2-yloxy-1H-pyrazol-3-amine
121507-34-4

5-propan-2-yloxy-1H-pyrazol-3-amine

2,6-dicholoro-3-nitropyridine
16013-85-7

2,6-dicholoro-3-nitropyridine

6-chloro-N-(5-isopropoxy-1H-pyrazol-3-yl)-3-nitropyridin-2-amine
905587-12-4

6-chloro-N-(5-isopropoxy-1H-pyrazol-3-yl)-3-nitropyridin-2-amine

Conditions
ConditionsYield
With triethylamine In acetonitrile at 20℃; for 24h;95%
With N-ethyl-N,N-diisopropylamine In tetrahydrofuran at 0 - 60℃; for 96h;63%
With N-ethyl-N,N-diisopropylamine In tetrahydrofuran at 25 - 60℃; for 72h;59%
With triethylamine In acetonitrile at 20℃; for 24h;
2,6-dicholoro-3-nitropyridine
16013-85-7

2,6-dicholoro-3-nitropyridine

tert-butyl alcohol
75-65-0

tert-butyl alcohol

C9H11ClN2O3
1094235-39-8

C9H11ClN2O3

Conditions
ConditionsYield
With sodium hydride In toluene at 60℃; for 0.5h; Inert atmosphere; regioselective reaction;95%
Stage #1: tert-butyl alcohol With sodium hydride In toluene at 0℃; Inert atmosphere;
Stage #2: 2,6-dicholoro-3-nitropyridine In toluene at 20℃; Inert atmosphere;
2,6-dicholoro-3-nitropyridine
16013-85-7

2,6-dicholoro-3-nitropyridine

1,4-phenylenediamine
106-50-3

1,4-phenylenediamine

2-(4-aminophenylamino)-6-chloro-3-nitropyridine

2-(4-aminophenylamino)-6-chloro-3-nitropyridine

Conditions
ConditionsYield
With triethylamine In methanol at 0 - 5℃; for 2h;95%
With triethylamine In methanol at 0 - 5℃; for 2h;95%
2,6-dicholoro-3-nitropyridine
16013-85-7

2,6-dicholoro-3-nitropyridine

4-chloro-aniline
106-47-8

4-chloro-aniline

6-chloro-N-(4-chlorophenyl)-3-nitropyridin-2-amine
1097004-77-7

6-chloro-N-(4-chlorophenyl)-3-nitropyridin-2-amine

Conditions
ConditionsYield
With N-ethyl-N,N-diisopropylamine In 1,4-dioxane at 80℃; for 3h;95%
With potassium carbonate In tert-butyl alcohol at 180℃; for 0.333333h; Microwave irradiation;76%
2,6-dicholoro-3-nitropyridine
16013-85-7

2,6-dicholoro-3-nitropyridine

N-tert-butoxycarbonyl-3-aminopropanol
58885-58-8

N-tert-butoxycarbonyl-3-aminopropanol

helical-1

helical-1

Conditions
ConditionsYield
Stage #1: 2,6-dicholoro-3-nitropyridine; N-tert-butoxycarbonyl-3-aminopropanol In toluene at 0℃; for 0.25h; Inert atmosphere;
Stage #2: With sodium hydride In toluene; mineral oil at 0 - 20℃; for 4.83333h; Inert atmosphere;
95%
With sodium hydride In toluene; mineral oil at 0 - 20℃; for 4.5h;95%
1-amino-3-methylbutane
107-85-7

1-amino-3-methylbutane

2,6-dicholoro-3-nitropyridine
16013-85-7

2,6-dicholoro-3-nitropyridine

6-chloro-N-isopentyl-3-nitropyridin-2-amine
1094388-67-6

6-chloro-N-isopentyl-3-nitropyridin-2-amine

Conditions
ConditionsYield
With triethylamine In tert-butyl methyl ether at -5 - 20℃; Inert atmosphere;94.2%
2,6-dicholoro-3-nitropyridine
16013-85-7

2,6-dicholoro-3-nitropyridine

(1R)-1-[2-bromo-6-(difluoromethoxy)phenyl]but-3-en-1-amine

(1R)-1-[2-bromo-6-(difluoromethoxy)phenyl]but-3-en-1-amine

N-{(1R)-1-[2-bromo-6-(difluoromethoxy)phenyl]but-3-en-1-yl}-6-chloro-3-nitropyridin-2-amine

N-{(1R)-1-[2-bromo-6-(difluoromethoxy)phenyl]but-3-en-1-yl}-6-chloro-3-nitropyridin-2-amine

Conditions
ConditionsYield
With triethylamine In dichloromethane Inert atmosphere;94%
2,6-dicholoro-3-nitropyridine
16013-85-7

2,6-dicholoro-3-nitropyridine

2-amino-6-chloro-3-nitropyridine
27048-04-0

2-amino-6-chloro-3-nitropyridine

Conditions
ConditionsYield
With ammonia In ethanol at 0℃; for 3h;93.6%
Stage #1: 2,6-dicholoro-3-nitropyridine With ammonia In ethanol at 0℃; for 3h;
Stage #2: In ethanol at 20℃; for 16h; Sealed tube;
93.6%
With ammonia In ethanol at 0 - 20℃;92%
2,6-dicholoro-3-nitropyridine
16013-85-7

2,6-dicholoro-3-nitropyridine

2,6-diamino-3-nitro-pyridine
3346-63-2

2,6-diamino-3-nitro-pyridine

Conditions
ConditionsYield
With copper(l) iodide; ammonia In water; N,N-dimethyl-formamide at 135℃; for 3h; Sealed tube; Microwave irradiation;93%
With zinc ammonium chloride at 220℃; for 5h; Autoclave;78%
Multi-step reaction with 2 steps
1: ammonium hydroxide / isopropyl alcohol / 120 h / 35 °C
2: ammonium hydroxide / ethanol / 2 h / 140 °C
View Scheme
1-methyl-piperazine
109-01-3

1-methyl-piperazine

2,6-dicholoro-3-nitropyridine
16013-85-7

2,6-dicholoro-3-nitropyridine

6-chloro-2-(4-methyl-1-piperazinyl)-3-nitropyridine
148927-24-6

6-chloro-2-(4-methyl-1-piperazinyl)-3-nitropyridine

Conditions
ConditionsYield
In toluene for 5h; Ambient temperature;92%
2,6-dicholoro-3-nitropyridine
16013-85-7

2,6-dicholoro-3-nitropyridine

methylamine
74-89-5

methylamine

6-chloro-N-methyl-3-nitropyridin-2-amine
33742-70-0

6-chloro-N-methyl-3-nitropyridin-2-amine

Conditions
ConditionsYield
With sodium carbonate In ethanol at 0 - 20℃;92%
With sodium carbonate In ethanol at 20℃; for 8h; Amination;86%
With sodium carbonate In methanol; ethanol at 20℃; for 3h;82%
2,6-dicholoro-3-nitropyridine
16013-85-7

2,6-dicholoro-3-nitropyridine

1-amino-2-propene
107-11-9

1-amino-2-propene

N-allyl-6-chloro-3-nitropyridin-2-amine
874286-20-1

N-allyl-6-chloro-3-nitropyridin-2-amine

Conditions
ConditionsYield
With triethylamine In dichloromethane at -15 - 20℃; for 16h;92%
With triethylamine In dichloromethane at -15 - 20℃;85%
With triethylamine In dichloromethane at -15 - 20℃; Inert atmosphere;85%
Stage #1: 1-amino-2-propene With sodium hydride In toluene at 0℃; Inert atmosphere;
Stage #2: 2,6-dicholoro-3-nitropyridine In toluene at 20℃; Inert atmosphere;

16013-85-7Relevant articles and documents

Optimization of 4,6-Disubstituted Pyrido[3,2-d]pyrimidines as Dual MNK/PIM Inhibitors to Inhibit Leukemia Cell Growth

Han, Yu,Zhang, Huimin,Wang, Shuxiang,Li, Bo,Xing, Kun,Shi, Yuntao,Cao, Hongxue,Zhang, Jian,Tong, Tong,Zang, Jie,Guan, Lihong,Gao, Xiaoxiao,Wang, Yuetong,Liu, Dan,Huang, Min,Jing, Yongkui,Zhao, Linxiang

, p. 13719 - 13735 (2021/10/01)

Mitogen-activated protein kinase-interacting kinases (MNKs) and provirus integration in maloney murine leukemia virus kinases (PIMs) are downstream enzymes of cell proliferation signaling pathways associated with the resistance of tyrosine kinase inhibitors. MNKs and PIMs have complementary effects to regulate cap-dependent translation of oncoproteins. Dual inhibitors of MNKs and PIMs have not been developed. We developed a novel 4,6-disubstituted pyrido[3,2-d]pyrimidine compound 21o with selective inhibition of MNKs and PIMs. The IC50’s of 21o to inhibit MNK1 and MNK2 are 1 and 7 nM and those to inhibit PIM1, PIM2, and PIM3 are 43, 232, and 774 nM, respectively. 21o inhibits the growth of myeloid leukemia K562 and MOLM-13 cells with GI50’s of 2.1 and 1.2 μM, respectively. 21o decreases the levels ofp-eIF4E andp-4EBP1, the downstream products of MNKs and PIMs, as well as cap-dependent proteins c-myc, cyclin D1, and Mcl-1. 21o inhibits the growth of MOLM-13 cell xenografts without causing evident toxicity. 21o represents an innovative dual MNK/PIM inhibitor with a good pharmacokinetic profile.

NITRATION

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Page/Page column 36; 37; 49; 39; 53, (2020/05/28)

The present invention relates to a process for preparing a nitrated compound, comprising the step of reacting a compound (A) comprising at least one substituted or unsubstituted aromatic or heteroaromatic ring, wherein said heteroaromatic ring comprises at least one heteroatom selected from the group consisting of oxygen, sulfur, phosphor, selenium and nitrogen, with a compound of formula (I) wherein Y is selected from the group consisting of hydrogen and nitro.

Preparation method of 2,6-dichloro-3-nitropyridine

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Paragraph 0040-0045, (2019/10/01)

The invention relates to a 2,6-Dichloro-3-Preparation method of nitropyridine. The method uses 2-Nitroacetate and 2-Halogenated acrylates are catalyzed by organic bases for 1,4-Addition reaction followed by cyclization reaction with ammonia to obtain 2,6-Dihydroxy-3-Nitropyridine is then reacted with a chlorinating reagent to produce 2,6-Dichloro-3-Nitropyridine. The invention does not use concentrated sulfuric acid and nitric acid, the used raw materials are cheap and easily available, the operation is simple and convenient, the conditions are mild, the amount of waste water is small, the invention is safe and environment-friendly and the cost is low.

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