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4-Bromo-5-fluoro-2-nitrotoluene is a chemical with a specific purpose. Lookchem provides you with multiple data and supplier information of this chemical.

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  • 224185-19-7 Structure
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    1. Product Name: 4-Bromo-5-fluoro-2-nitrotoluene
    2. Synonyms: 4-BROMO-3-FLUORO-6-NITROTOLUENE;4-BROMO-5-FLUORO-2-NITROTOLUENE;4-Bromo-5-fluoro-2-nitortoluene;2-Nitro-4-Bromo-5-Fluorotoluene;1-Bromo-2-fluoro-4-methyl-5-nitro-benzene;Benzene,1-broMo-2-fluoro-4-Methyl-5-nitro-
    3. CAS NO:224185-19-7
    4. Molecular Formula: C7H5BrFNO2
    5. Molecular Weight: 234.02
    6. EINECS: 1533716-785-6
    7. Product Categories: Aromatic Hydrocarbons (substituted) & Derivatives;Halogen toluene;Miscellaneous;Nitro Compounds;Nitrogen Compounds;Organic Building Blocks
    8. Mol File: 224185-19-7.mol
  • Chemical Properties

    1. Melting Point: 59-63°C
    2. Boiling Point: 266.6 °C at 760 mmHg
    3. Flash Point: 115.1 °C
    4. Appearance: /
    5. Density: 1.696 g/cm3
    6. Vapor Pressure: 0.0141mmHg at 25°C
    7. Refractive Index: 1.57
    8. Storage Temp.: Sealed in dry,Room Temperature
    9. Solubility: N/A
    10. CAS DataBase Reference: 4-Bromo-5-fluoro-2-nitrotoluene(CAS DataBase Reference)
    11. NIST Chemistry Reference: 4-Bromo-5-fluoro-2-nitrotoluene(224185-19-7)
    12. EPA Substance Registry System: 4-Bromo-5-fluoro-2-nitrotoluene(224185-19-7)
  • Safety Data

    1. Hazard Codes: Xn,Xi
    2. Statements: 22-36-36/37/38
    3. Safety Statements: 26-36/37-36
    4. WGK Germany: 3
    5. RTECS:
    6. HazardClass: N/A
    7. PackingGroup: N/A
    8. Hazardous Substances Data: 224185-19-7(Hazardous Substances Data)

224185-19-7 Usage

Chemical Properties

pale yellow powder

Check Digit Verification of cas no

The CAS Registry Mumber 224185-19-7 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 2,2,4,1,8 and 5 respectively; the second part has 2 digits, 1 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 224185-19:
(8*2)+(7*2)+(6*4)+(5*1)+(4*8)+(3*5)+(2*1)+(1*9)=117
117 % 10 = 7
So 224185-19-7 is a valid CAS Registry Number.
InChI:InChI=1/C7H5BrFNO2/c1-4-2-6(9)5(8)3-7(4)10(11)12/h2-3H,1H3

224185-19-7 Well-known Company Product Price

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  • Alfa Aesar

  • (H27552)  4-Bromo-5-fluoro-2-nitrotoluene, 98%   

  • 224185-19-7

  • 1g

  • 362.0CNY

  • Detail
  • Alfa Aesar

  • (H27552)  4-Bromo-5-fluoro-2-nitrotoluene, 98%   

  • 224185-19-7

  • 5g

  • 1264.0CNY

  • Detail
  • Aldrich

  • (638994)  4-Bromo-5-fluoro-2-nitrotoluene  97%

  • 224185-19-7

  • 638994-5G

  • 1,144.26CNY

  • Detail

224185-19-7SDS

SAFETY DATA SHEETS

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

Version: 1.0

Creation Date: Aug 19, 2017

Revision Date: Aug 19, 2017

1.Identification

1.1 GHS Product identifier

Product name 1-bromo-2-fluoro-4-methyl-5-nitrobenzene

1.2 Other means of identification

Product number -
Other names 4-Bromo-5-Fluoro-2-Nitrotoluene

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:224185-19-7 SDS

224185-19-7Synthetic route

4-bromo-3-fluorotoluene
452-74-4

4-bromo-3-fluorotoluene

3-bromo-4-fluoro-6-methylnitrobenzene
224185-19-7

3-bromo-4-fluoro-6-methylnitrobenzene

Conditions
ConditionsYield
With sulfuric acid; potassium nitrate at 0 - 20℃;100%
With sulfuric acid; potassium nitrate at 0℃;100%
With sulfuric acid; nitric acid at 0℃;92%
2-fluoro-4-methyl-5-nitro-phenylamine
259860-00-9

2-fluoro-4-methyl-5-nitro-phenylamine

3-bromo-4-fluoro-6-methylnitrobenzene
224185-19-7

3-bromo-4-fluoro-6-methylnitrobenzene

Conditions
ConditionsYield
Stage #1: 2-fluoro-4-methyl-5-nitro-phenylamine With hydrogen bromide; sodium nitrite In water at 0 - 5℃; for 0.25h;
Stage #2: With copper(I) oxide; hydrogen bromide In water at 0℃;
91%
3-fluoro-6-nitrotoluene
446-33-3

3-fluoro-6-nitrotoluene

3-bromo-4-fluoro-6-methylnitrobenzene
224185-19-7

3-bromo-4-fluoro-6-methylnitrobenzene

Conditions
ConditionsYield
With sulfuric acid; bromine; silver nitrate In (2S)-N-methyl-1-phenylpropan-2-amine hydrate83%
copper(I) bromide
7787-70-4

copper(I) bromide

2-fluoro-4-methyl-5-nitro-phenylamine
259860-00-9

2-fluoro-4-methyl-5-nitro-phenylamine

3-bromo-4-fluoro-6-methylnitrobenzene
224185-19-7

3-bromo-4-fluoro-6-methylnitrobenzene

Conditions
ConditionsYield
With sodium nitrite In water; hydrogen bromide50%
sodium ethanolate
141-52-6

sodium ethanolate

3-bromo-4-fluoro-6-methylnitrobenzene
224185-19-7

3-bromo-4-fluoro-6-methylnitrobenzene

1-bromo-2-ethoxy-4-methyl-5-nitrobenzene
1226903-38-3

1-bromo-2-ethoxy-4-methyl-5-nitrobenzene

Conditions
ConditionsYield
With sodium ethanolate In ethanol at 20℃; for 1h;99%
1-methyl-5-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-1H-pyridin-2-one
1002309-52-5

1-methyl-5-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-1H-pyridin-2-one

3-bromo-4-fluoro-6-methylnitrobenzene
224185-19-7

3-bromo-4-fluoro-6-methylnitrobenzene

5-(2-fluoro-4-methyl-5-nitrophenyl)-1-methylpyridin-2(1H)-one

5-(2-fluoro-4-methyl-5-nitrophenyl)-1-methylpyridin-2(1H)-one

Conditions
ConditionsYield
With bis-triphenylphosphine-palladium(II) chloride; sodium carbonate In 1,2-dimethoxyethane; water at 120℃; for 0.5h; Suzuki Coupling; Inert atmosphere; Microwave irradiation;99%
With bis-triphenylphosphine-palladium(II) chloride; sodium carbonate In 1,2-dimethoxyethane; water at 120℃; for 0.5h; Inert atmosphere; Microwave irradiation;99%
2,4-difluorophenol
367-27-1

2,4-difluorophenol

3-bromo-4-fluoro-6-methylnitrobenzene
224185-19-7

3-bromo-4-fluoro-6-methylnitrobenzene

1-bromo-2-(2,4-difluorophenoxy)-4-methyl-5-nitrobenzene

1-bromo-2-(2,4-difluorophenoxy)-4-methyl-5-nitrobenzene

Conditions
ConditionsYield
With potassium carbonate In dimethyl sulfoxide at 20℃;99%
With caesium carbonate In dimethyl sulfoxide at 100℃; for 3h;3.8 g
3-bromo-4-fluoro-6-methylnitrobenzene
224185-19-7

3-bromo-4-fluoro-6-methylnitrobenzene

5-bromo-4-fluoro-2-methylaniline
627871-16-3

5-bromo-4-fluoro-2-methylaniline

Conditions
ConditionsYield
With 2,3-dimethyl-2,3-butane diol; [MoO2Cl2(dmf)2] In o-xylene at 130℃; for 3h; chemoselective reaction;95%
With iron; ammonium chloride In water for 48.5h; Heating / reflux;72%
With ammonium chloride; iron In water for 48h; Heating / reflux;72%
bis(pinacol)diborane
73183-34-3

bis(pinacol)diborane

3-bromo-4-fluoro-6-methylnitrobenzene
224185-19-7

3-bromo-4-fluoro-6-methylnitrobenzene

2-(2-fluoro-4-methyl-5-nitrophenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane
1510828-68-8

2-(2-fluoro-4-methyl-5-nitrophenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane

Conditions
ConditionsYield
With [1,1'-bis(diphenylphosphino)-ferrocene]palladium(II) chloride-dichlormethane complex; potassium acetate In 1,4-dioxane at 100℃; for 1h; Suzuki Coupling; Inert atmosphere; Sealed tube;91%
With dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II)*CH2Cl2; potassium acetate In 1,4-dioxane at 90℃; for 15h; Inert atmosphere;
methanol
67-56-1

methanol

3-bromo-4-fluoro-6-methylnitrobenzene
224185-19-7

3-bromo-4-fluoro-6-methylnitrobenzene

1-bromo-2-methoxy-4-methyl-5-nitrobenzene
861076-28-0

1-bromo-2-methoxy-4-methyl-5-nitrobenzene

Conditions
ConditionsYield
Stage #1: methanol With sodium at 0℃; for 0.5h;
Stage #2: 3-bromo-4-fluoro-6-methylnitrobenzene at 30℃; for 2h;
87.8%
With sodium at 40℃; for 2h; Cooling with ice;
3-bromo-4-fluoro-6-methylnitrobenzene
224185-19-7

3-bromo-4-fluoro-6-methylnitrobenzene

N-(5-bromo-4-fluoro-2-methylphenyl)iminodiacetic acid diethyl ester
1190892-54-6

N-(5-bromo-4-fluoro-2-methylphenyl)iminodiacetic acid diethyl ester

Conditions
ConditionsYield
85%
N,N-dimethyl-formamide dimethyl acetal
4637-24-5

N,N-dimethyl-formamide dimethyl acetal

3-bromo-4-fluoro-6-methylnitrobenzene
224185-19-7

3-bromo-4-fluoro-6-methylnitrobenzene

[2-(4-bromo-5-fluoro-2-nitro-phenyl)-vinyl]-dimethyl-amine
1034894-73-9

[2-(4-bromo-5-fluoro-2-nitro-phenyl)-vinyl]-dimethyl-amine

Conditions
ConditionsYield
In N,N-dimethyl-formamide at 125℃; for 3h;83%
morpholine
110-91-8

morpholine

3-bromo-4-fluoro-6-methylnitrobenzene
224185-19-7

3-bromo-4-fluoro-6-methylnitrobenzene

4-(2-bromo-5-methyl-4-nitrophenyl)morpholine
1192471-65-0

4-(2-bromo-5-methyl-4-nitrophenyl)morpholine

Conditions
ConditionsYield
With potassium carbonate In N,N-dimethyl-formamide for 3h;77%
With potassium carbonate In N,N-dimethyl-formamide at 25℃; for 0.5h;5.7 g
2-amino-phenol
95-55-6

2-amino-phenol

3-bromo-4-fluoro-6-methylnitrobenzene
224185-19-7

3-bromo-4-fluoro-6-methylnitrobenzene

3-methyl-2-nitro-10H-phenoxazine

3-methyl-2-nitro-10H-phenoxazine

Conditions
ConditionsYield
In dimethyl sulfoxide at 120℃; for 24h;62%
2-Hydroxy-4-methylanilin
2835-98-5

2-Hydroxy-4-methylanilin

3-bromo-4-fluoro-6-methylnitrobenzene
224185-19-7

3-bromo-4-fluoro-6-methylnitrobenzene

C14H12N2O3

C14H12N2O3

Conditions
ConditionsYield
In dimethyl sulfoxide at 120℃; for 24h;60%
3-amino-4-hydroxytoluene
95-84-1

3-amino-4-hydroxytoluene

3-bromo-4-fluoro-6-methylnitrobenzene
224185-19-7

3-bromo-4-fluoro-6-methylnitrobenzene

C14H12N2O3

C14H12N2O3

Conditions
ConditionsYield
In dimethyl sulfoxide at 120℃; for 24h;57%
2-hydroxy-5-chloro-aniline
95-85-2

2-hydroxy-5-chloro-aniline

3-bromo-4-fluoro-6-methylnitrobenzene
224185-19-7

3-bromo-4-fluoro-6-methylnitrobenzene

C13H9ClN2O3

C13H9ClN2O3

Conditions
ConditionsYield
In dimethyl sulfoxide at 120℃; for 24h;52%
3-bromo-4-fluoro-6-methylnitrobenzene
224185-19-7

3-bromo-4-fluoro-6-methylnitrobenzene

C7H4Br2FNO2

C7H4Br2FNO2

Conditions
ConditionsYield
With N-Bromosuccinimide; 2,2'-azobis(isobutyronitrile) In tetrachloromethane for 16h; Reflux;50%
o-(N-methylamino)phenol
611-24-5

o-(N-methylamino)phenol

3-bromo-4-fluoro-6-methylnitrobenzene
224185-19-7

3-bromo-4-fluoro-6-methylnitrobenzene

C14H12N2O3

C14H12N2O3

Conditions
ConditionsYield
In dimethyl sulfoxide at 120℃; for 24h;48%
tert-butyl 2-((2S,6R)-4-(2-hydroxyethyl)-2,6-dimethylpiperazin-1-yl)acetate

tert-butyl 2-((2S,6R)-4-(2-hydroxyethyl)-2,6-dimethylpiperazin-1-yl)acetate

3-bromo-4-fluoro-6-methylnitrobenzene
224185-19-7

3-bromo-4-fluoro-6-methylnitrobenzene

tert-butyl 2-((2S,6R)-4-(2-(2-bromo-5-methyl-4-nitrophenoxy)ethyl)-2,6-dimethylpiperazin-1-yl)acetate

tert-butyl 2-((2S,6R)-4-(2-(2-bromo-5-methyl-4-nitrophenoxy)ethyl)-2,6-dimethylpiperazin-1-yl)acetate

Conditions
ConditionsYield
Stage #1: tert-butyl 2-((2S,6R)-4-(2-hydroxyethyl)-2,6-dimethylpiperazin-1-yl)acetate With sodium t-butanolate In tetrahydrofuran at 0℃; for 1h;
Stage #2: 3-bromo-4-fluoro-6-methylnitrobenzene In tetrahydrofuran at 15℃; for 1h; Temperature;
44.4%
cyclohexanol
108-93-0

cyclohexanol

3-bromo-4-fluoro-6-methylnitrobenzene
224185-19-7

3-bromo-4-fluoro-6-methylnitrobenzene

1-bromo-2-(cyclohexyloxy)-4-methyl-5-nitrobenzene
1351812-80-0

1-bromo-2-(cyclohexyloxy)-4-methyl-5-nitrobenzene

Conditions
ConditionsYield
With potassium hydroxide In acetonitrile at 0 - 20℃; for 22h; Suzuki Coupling;36%
aluminum nickel

aluminum nickel

N,N-dimethyl-formamide dimethyl acetal
4637-24-5

N,N-dimethyl-formamide dimethyl acetal

3-bromo-4-fluoro-6-methylnitrobenzene
224185-19-7

3-bromo-4-fluoro-6-methylnitrobenzene

6-bromo-5-fluoro-1H-indole
259860-08-7

6-bromo-5-fluoro-1H-indole

Conditions
ConditionsYield
With hydrazine hydrate In tetrahydrofuran; methanol; N,N-dimethyl-formamide16%
3-bromo-4-fluoro-6-methylnitrobenzene
224185-19-7

3-bromo-4-fluoro-6-methylnitrobenzene

5-bromo-4-fluoro-2-methylbenzenethiol
873922-26-0

5-bromo-4-fluoro-2-methylbenzenethiol

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1.1: 63 percent / SnCl2 / ethyl acetate
2.1: NaNO2; aq. HCl
2.2: potassium ethyl xanthogenate
2.3: 92 percent / KOH / ethanol
View Scheme
3-bromo-4-fluoro-6-methylnitrobenzene
224185-19-7

3-bromo-4-fluoro-6-methylnitrobenzene

4-bromo-5-fluoro-7-methyl-benzo[b]thiophen-3-one
873922-28-2

4-bromo-5-fluoro-7-methyl-benzo[b]thiophen-3-one

Conditions
ConditionsYield
Multi-step reaction with 6 steps
1.1: 63 percent / SnCl2 / ethyl acetate
2.1: NaNO2; aq. HCl
2.2: potassium ethyl xanthogenate
2.3: 92 percent / KOH / ethanol
3.1: pyridine / 0 °C
4.1: TFA / CH2Cl2
5.1: SOCl2 / 90 °C
6.1: AlCl3 / chlorobenzene
View Scheme
3-bromo-4-fluoro-6-methylnitrobenzene
224185-19-7

3-bromo-4-fluoro-6-methylnitrobenzene

(5-bromo-4-fluoro-2-methyl-phenylsulfanyl)-acetyl chloride

(5-bromo-4-fluoro-2-methyl-phenylsulfanyl)-acetyl chloride

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1.1: 63 percent / SnCl2 / ethyl acetate
2.1: NaNO2; aq. HCl
2.2: potassium ethyl xanthogenate
2.3: 92 percent / KOH / ethanol
3.1: pyridine / 0 °C
4.1: TFA / CH2Cl2
5.1: SOCl2 / 90 °C
View Scheme
3-bromo-4-fluoro-6-methylnitrobenzene
224185-19-7

3-bromo-4-fluoro-6-methylnitrobenzene

(5-bromo-4-fluoro-2-methyl-phenylsulfanyl)-acetic acid
873922-27-1

(5-bromo-4-fluoro-2-methyl-phenylsulfanyl)-acetic acid

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1.1: 63 percent / SnCl2 / ethyl acetate
2.1: NaNO2; aq. HCl
2.2: potassium ethyl xanthogenate
2.3: 92 percent / KOH / ethanol
3.1: pyridine / 0 °C
4.1: TFA / CH2Cl2
View Scheme
3-bromo-4-fluoro-6-methylnitrobenzene
224185-19-7

3-bromo-4-fluoro-6-methylnitrobenzene

2-(4-bromo-5-fluoro-7-methyl-benzo[b]thiophen-3-yl)-ethanol
845746-23-8

2-(4-bromo-5-fluoro-7-methyl-benzo[b]thiophen-3-yl)-ethanol

Conditions
ConditionsYield
Multi-step reaction with 8 steps
1.1: 63 percent / SnCl2 / ethyl acetate
2.1: NaNO2; aq. HCl
2.2: potassium ethyl xanthogenate
2.3: 92 percent / KOH / ethanol
3.1: pyridine / 0 °C
4.1: TFA / CH2Cl2
5.1: SOCl2 / 90 °C
6.1: AlCl3 / chlorobenzene
7.1: 39 percent / toluene / 120 °C
8.1: 83 percent / LiAlH4 / tetrahydrofuran / 0 °C
View Scheme
3-bromo-4-fluoro-6-methylnitrobenzene
224185-19-7

3-bromo-4-fluoro-6-methylnitrobenzene

(5-bromo-4-fluoro-2-methyl-phenylsulfanyl)-acetic acid tert-butyl ester

(5-bromo-4-fluoro-2-methyl-phenylsulfanyl)-acetic acid tert-butyl ester

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1.1: 63 percent / SnCl2 / ethyl acetate
2.1: NaNO2; aq. HCl
2.2: potassium ethyl xanthogenate
2.3: 92 percent / KOH / ethanol
3.1: pyridine / 0 °C
View Scheme
3-bromo-4-fluoro-6-methylnitrobenzene
224185-19-7

3-bromo-4-fluoro-6-methylnitrobenzene

(4-bromo-5-fluoro-7-methyl-benzo[b]thiophen-3-yl)-acetic acid ethyl ester
873922-29-3

(4-bromo-5-fluoro-7-methyl-benzo[b]thiophen-3-yl)-acetic acid ethyl ester

Conditions
ConditionsYield
Multi-step reaction with 7 steps
1.1: 63 percent / SnCl2 / ethyl acetate
2.1: NaNO2; aq. HCl
2.2: potassium ethyl xanthogenate
2.3: 92 percent / KOH / ethanol
3.1: pyridine / 0 °C
4.1: TFA / CH2Cl2
5.1: SOCl2 / 90 °C
6.1: AlCl3 / chlorobenzene
7.1: 39 percent / toluene / 120 °C
View Scheme
3-bromo-4-fluoro-6-methylnitrobenzene
224185-19-7

3-bromo-4-fluoro-6-methylnitrobenzene

(5-cyano-6-fluoro-8-methyl-1-propyl-3,4-dihydro-1H-[1]benzothieno[2,3-c]pyran-1-yl)acetic acid
845746-06-7

(5-cyano-6-fluoro-8-methyl-1-propyl-3,4-dihydro-1H-[1]benzothieno[2,3-c]pyran-1-yl)acetic acid

Conditions
ConditionsYield
Multi-step reaction with 11 steps
1.1: 63 percent / SnCl2 / ethyl acetate
2.1: NaNO2; aq. HCl
2.2: potassium ethyl xanthogenate
2.3: 92 percent / KOH / ethanol
3.1: pyridine / 0 °C
4.1: TFA / CH2Cl2
5.1: SOCl2 / 90 °C
6.1: AlCl3 / chlorobenzene
7.1: 39 percent / toluene / 120 °C
8.1: 83 percent / LiAlH4 / tetrahydrofuran / 0 °C
9.1: 75 percent / BF3-Et2O / CH2Cl2
10.1: NMP / 0.25 h / 220 °C / microwave irradiation
11.1: aq. NaOH / ethanol; tetrahydrofuran
View Scheme

224185-19-7Relevant articles and documents

Aromatic amine derivative organic electroluminescent material and device thereof

-

Paragraph 0252-0255, (2021/11/26)

The invention discloses an aromatic amine derivative organic electroluminescent material and a device thereof. The compound is a pyrene compound substituted with an aromatic amine, wherein the compound has a substituted or unsubstituted (hetero) aryl group and a pyrene compound substituted or unsubstituted aromatic amine structure of a (hetero) aryl group, which may be used as a light emitting material in an organic electroluminescent device. These novel compounds can provide better device performance, such as higher external quantum efficiency and narrower half-peak widths, and the like.

HEPARAN SULFATE BIOSYNTHESIS INHIBITORS FOR THE TREATMENT OF DISEASES

-

Paragraph 000891, (2016/05/02)

Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions in need of inhibition of heparan sulfate biosynthesis.

INHIBITORS OF KRAS G12C

-

Page/Page column 247, (2015/04/28)

Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, tautomer, prodrug or stereoisomer thereof, wherein R1, R2a, R3a, R3b, R4a, R4b, G1, G2, L1, L2, m1, m2, A, B, W, X, Y, Z and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

3-BENZOFURANYL-4-INDOLYL MALEIMIDES AS POTENT GSK3 INHIBITORS FOR NEUROGENERATIVE DISORDERS

-

Page/Page column 76, (2008/12/06)

Compounds of formula (I): and pharmaceutically acceptable salts, esters and solvates thereof, where variables are defined in the specification, useful generally as inhibitors of protein kinases and particularly useful for inhibition of GSK-3. Pharmaceutically compositions and medicaments containing a compound of the invention are provided. The invention provides methods of treatment of protein kinase-related disease, disorders or conditions. The invention provides methods of treatment of GSK-3-related diseases, disorders or conditions. More specifically, methods of treatment of bipolar disorder, including mania, schizophrenia, stroke, epilepsy, motor neuron disease, cranial or spinal trauma, neurodegenerative disorders, including multiple sclerosis (MS), Alzheimer's disease, Fragile X syndrome, autism, Huntington's disease, Parkinson's

Design and synthesis of 3,4-dihydro-1H-[1]-benzothieno[2,3-c]pyran and 3,4-dihydro-1H-pyrano[3,4-b]benzofuran derivatives as non-nucleoside inhibitors of HCV NS5B RNA dependent RNA polymerase

Gopalsamy, Ariamala,Aplasca, Alexis,Ciszewski, Gregory,Park, Kaapjoo,Ellingboe, John W.,Orlowski, Mark,Feld, Boris,Howe, Anita Y.M.

, p. 457 - 460 (2007/10/03)

A novel class of HCV NS5B RNA dependent RNA polymerase inhibitors containing 3,4-dihydro-1H-[1]-benzothieno[2,3-c]pyran and 3,4-dihydro-1H- pyrano[3,4-b]benzofuran scaffolds were designed and synthesized. Optimization of the alkyl substituent in the pyran ring showed preference for an n-propyl group, while 5,8-disubstitution pattern is preferred for the aromatic region. Analog 19 displayed potent activity with an IC50 of 50 nM against HCV NS5B enzyme and was selective over a panel of polymerases.

Substituted indoles as alpha-1 agonists

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Page 21, (2010/02/09)

This invention relates to compounds which are alpha-1 receptor agonists, preferably alpha-1A/L receptor agonists, and which are represented by Formula I: wherein m, A, X, Y, R1, R2, R3, R4 and R5 are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.

R-ENANTIOMERS OF PYRANOINDOLE DERIVATIVES AGAINST HEPATITIS C

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Page 32, (2008/06/13)

The invention is directed to a compound and a pharmaceutical composition of the formula: Wherein substitutions at R1, R2, R3 - R12, and Y are set forth in the specification.

METHOD FOR THE USE OF PYRANOINDOLE DERIVATIVES TO TREAT INFECTION WITH HEPATITIS C VIRUS

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Page 65, (2008/06/13)

The invention is directed to methods of treating, preventing, or inhibiting a Hepatitis C viral infection in a mammal comprising containing the mammal with an effective amount of a compound of the formula: Wherein substitutions at R1, R2, R3-R12, and Y are set forth in the specification.

Indoline derivatives as 5-HT2B and or 5-HTC receptor ligands

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, (2008/06/13)

For use in therapy a chemical compound of formula (I), wherein R1to R3are independently selected from hydrogen and alkyl; R4to R7are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, heterocyclyl, alkoxy, aryloxy, alkylthio, arylthio, alkylsulfoxyl, alkylsulfonyl, arylsulfoxyl, arylsulfonyl, amino, monoalkylamino, dialkylamino, nitro, cyano, carboxaldehyde, alkylcarbonyl, arylcarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkoxycarbonylamino, aminocarbonyloxy, monoalkylaminocarbonyloxy, dialkylaminocarbonyloxy, monoalkylaminocarbonylamino and dialkylaminocarbonylamino, wherein at least one of R4to R7is a substituent group other than hydrogen, and pharmaceutically acceptable salts and prodrugs thereof, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apnea, and especially for the treatment of obesity; chemical compounds of formula (I) other than compounds wherein R7is hydroxy.

Heterocyclic compounds having nos inhibitory activities

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, (2008/06/13)

Compounds represented by the general formula (1): [wherein R1is typically an aminoalkyl group; R2is typically a hydrogen atom, a lower alkyl group, R3or SR4(where R4is typically a lower alkyl group); Ar is typically a 5-membered aromatic heterocyclic group] have an NOS inhibiting activity and are useful as therapeutics of cerebrovascular diseases and other pharmaceuticals.

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