1975-51-5

Basic information

• Product Name: 2-Methyl-4-nitrobenzoic acid
• Synonyms: 2-METHYL-4-NITROBENZOIC ACID 97;4-nitro-o-toluic acid;4-Nitro-2-methylbenzoicacid;2-Methyl-4-nitrobenzoic acid;2-Methyl-4-nitrobenz;4-Carboxy-3-methylnitrobenzene, 2-Carboxy-5-nitrotoluene;2-Methyl-4-nitro-benzoic acid 4-nitro-o-toluic acid;4-Carboxy-3-methylnitrobenzene, 2-Carboxy-5-nitrotoluene, 4-Nitro-o-toluic acid
• CAS NO: 1975-51-5
• Molecular Formula: C₈H₇NO₄
• Molecular Weight: 181.15
• EINECS: 217-828-5
• Product Categories: Carboxylic Acids;Phenyls & Phenyl-Het;C8;Carbonyl Compounds;Tolvaptan intermediate
• Mol File: 1975-51-5.mol

Chemical Properties

• Melting Point: 150-154 °C(lit.)
• Boiling Point: 369.3 °C at 760 mmHg
• Flash Point: 167.6 °C
• Appearance: /
• Density: 1.392 g/cm³
• Vapor Pressure: 4.19E-06mmHg at 25°C
• Refractive Index: 1.6
• Storage Temp.: Sealed in dry,Room Temperature
• Solubility: DMSO (Slightly), Methanol (Slightly)
• PKA: pK1:1.86 (25°C)
• CAS DataBase Reference: 2-Methyl-4-nitrobenzoic acid(CAS DataBase Reference)
• NIST Chemistry Reference: 2-Methyl-4-nitrobenzoic acid(1975-51-5)
• EPA Substance Registry System: 2-Methyl-4-nitrobenzoic acid(1975-51-5)

Safety Data

• Hazard Codes: Xn
• Statements: 22-43
• Safety Statements: 37/39
• WGK Germany: 3
• Hazardous Substances Data: 1975-51-5(Hazardous Substances Data)

Usage

Uses

Used in Pharmaceutical Industry:
2-Methyl-4-nitrobenzoic acid is used as a reagent for the synthesis of amino-1H-pyrazole amide derivatives, which are compounds that act as Raf kinase inhibitors in melanoma cells. These derivatives have potential applications in the development of targeted therapies for the treatment of melanoma and other cancers.
Used in Biotechnology Industry:
2-Methyl-4-nitrobenzoic acid is also used as a reagent to synthesize fluorogenic substrates, which are compounds that can be used for activity imaging within living cells. These substrates are valuable tools for studying enzyme activity, cellular processes, and other biological phenomena, as they allow for the visualization and quantification of specific cellular events in real-time.

InChI:InChI=1/C8H7NO4/c1-5-4-6(9(12)13)2-3-7(5)8(10)11/h2-4H,1H3,(H,10,11)

Synthetic route

4-nitro-o-xylene (99-51-4) → 2-methyl-4-nitrobenzoic acid (1975-51-5)

Conditions	Yield
With N-hydroxyphthalimide; cobalt(II) chloride hexahydrate; nitric acid; manganese (II) acetate tetrahydrate under 760.051 Torr; for 12h; Reagent/catalyst; Concentration; Reflux;	72%
With oxygen; sodium hydroxide In methanol; water at 65℃; under 13501.4 Torr; for 24h; Solvent; Temperature; Concentration; Autoclave;	62%
With oxygen; sodium hydroxide In ethanol; water at 60℃; under 7500.75 - 13501.4 Torr; for 24h; Solvent; Green chemistry; chemoselective reaction;	58%
With manganese(IV) oxide; nitric acid for 1h; Time;

2-methyl-4-nitro-benzoic acid amide (99584-16-4) → 2-methyl-4-nitrobenzoic acid (1975-51-5)

Conditions	Yield
With hydrogenchloride In water for 20h; Heating / reflux;	89.5%
With hydrogenchloride for 20h; Hydrolysis; Heating;	88%
With sulfuric acid; sodium nitrite

2-cyano-5-nitrotoluene (89001-53-6) → 2-methyl-4-nitrobenzoic acid (1975-51-5)

Conditions	Yield
With sodium hydroxide; dihydrogen peroxide In water Heating;	83%
With hydrogenchloride; acetic acid at 165℃;
With sodium hydroxide

palladium(II) dichloride bis(triphenylphosphine) + 2-iodo-3-nitrotoluene (6277-17-4) → 2-methyl-4-nitrobenzoic acid (1975-51-5)

Conditions	Yield
With potassium carbonate In diethyl ether; hexane; water; pyrographite; ethyl acetate; N,N-dimethyl-formamide
With potassium carbonate In diethyl ether; hexane; water; pyrographite; ethyl acetate; N,N-dimethyl-formamide
With potassium carbonate In diethyl ether; hexane; water; pyrographite; ethyl acetate; N,N-dimethyl-formamide

2-methyl-4-nitrobenzeneacetamide → 2-methyl-4-nitrobenzoic acid (1975-51-5)

Conditions	Yield
Stage #1: 2-methyl-4-nitrobenzeneacetamide With sodium hypochlorite; potassium permanganate at 80℃; for 0.666667h; Stage #2: With hydrogenchloride for 2h; Temperature;

4-amino-2-methylbenzoic acid (2486-75-1) → 2-methyl-4-nitrobenzoic acid (1975-51-5)

Conditions	Yield
With Streptomyces thioluteus para-aminobenzoate N-oxygenase

2-methyl-4-nitro-benzenamine (99-52-5) → 2-methyl-4-nitrobenzoic acid (1975-51-5)

Conditions	Yield
Multi-step reaction with 3 steps 1.1: aq. HCl; NaNO2 / 0 - 5 °C 1.2: 81 percent / KCN / ethyl acetate / 20 °C 2.1: 98 percent / 80 percent aq. H2SO4 / 1.25 h / 100 °C 3.1: 88 percent / 6 N aq. HCl / 20 h / Heating View Scheme
Multi-step reaction with 3 steps 1.1: 1 h / 60 °C 1.2: 2 h / 60 °C 2.1: dihydrogen peroxide; sodium perborate / 2 h / 300 °C / 22502.3 Torr 2.2: 0.83 h / 70 °C 3.1: potassium permanganate; sodium hypochlorite / 0.67 h / 80 °C 3.2: 2 h View Scheme

1-<2-methyl-4-nitro-phenyl>-propane-1,2-dione-1-oxime → 2-methyl-4-nitrobenzoic acid (1975-51-5)

Conditions	Yield
With hydrogenchloride; sulfuric acid at 120℃;

toluene (108-88-3) → 2-methyl-4-nitrobenzoic acid (1975-51-5)

Conditions	Yield
Multi-step reaction with 5 steps 1.1: nitric acid; sulfuric acid / toluene / 1.25 h / 20 - 65 °C 2.1: tin(ll) chloride; iron; acetic acid / 0.5 h / 85 °C 2.2: 0.83 h 3.1: 1 h / 60 °C 3.2: 2 h / 60 °C 4.1: dihydrogen peroxide; sodium perborate / 2 h / 300 °C / 22502.3 Torr 4.2: 0.83 h / 70 °C 5.1: potassium permanganate; sodium hypochlorite / 0.67 h / 80 °C 5.2: 2 h View Scheme

2-methyl-4-nitrobenzylpyridinium bromide (22162-16-9) → 2-methyl-4-nitrobenzoic acid (1975-51-5)

Conditions	Yield
With sodium hydroxide; bromine

asymm. nitro-o-xylene → 2-methyl-4-nitrobenzoic acid (1975-51-5) + 5-nitro-o-toluic acid (1975-52-6)

Conditions	Yield
With water; nitric acid
With nitric acid

2,5-dinitrotoluene (619-15-8) → 2-methyl-4-nitrobenzoic acid (1975-51-5)

Conditions	Yield
Multi-step reaction with 4 steps 1.1: tin(ll) chloride; iron; acetic acid / 0.5 h / 85 °C 1.2: 0.83 h 2.1: 1 h / 60 °C 2.2: 2 h / 60 °C 3.1: dihydrogen peroxide; sodium perborate / 2 h / 300 °C / 22502.3 Torr 3.2: 0.83 h / 70 °C 4.1: potassium permanganate; sodium hypochlorite / 0.67 h / 80 °C 4.2: 2 h View Scheme

4-nitro-o-xylene (99-51-4) + nitric acid (7697-37-2) → 2-methyl-4-nitrobenzoic acid (1975-51-5) + 5-nitro-o-toluic acid (1975-52-6)

hydrogenchloride (7647-01-0) + 2-cyano-5-nitrotoluene (89001-53-6) + acetic acid (64-19-7) → 2-methyl-4-nitrobenzoic acid (1975-51-5)

methanol (67-56-1) + 2-methyl-4-nitrobenzoic acid (1975-51-5) → methyl 2-methyl-4-nitrobenzoate (62621-09-4)

Conditions	Yield
With thionyl chloride at 70℃; for 4h;	100%
With thionyl chloride at 70℃; for 18h;	100%
With thionyl chloride at 20℃; for 21h; Esterification;	99%

2-methyl-4-nitrobenzoic acid (1975-51-5) + methyl iodide (74-88-4) → methyl 2-methyl-4-nitrobenzoate (62621-09-4)

Conditions	Yield
With potassium carbonate In N,N-dimethyl-formamide at 20℃; for 2h;	100%
With potassium carbonate In N,N-dimethyl-formamide at 20℃; for 2h;	98%
With potassium carbonate In N,N-dimethyl-formamide at 20℃; for 3h;	89%
With potassium carbonate In N,N-dimethyl-formamide at 0 - 20℃; for 4h;

2-methyl-4-nitrobenzoic acid (1975-51-5) + tert-butyl alcohol (75-65-0) → tert-butyl 4-amino-2-methylbenzoate

Conditions	Yield
Stage #1: 2-methyl-4-nitrobenzoic acid; tert-butyl alcohol With pyridine; p-toluenesulfonyl chloride at 0 - 20℃; Stage #2: With hydrogen; palladium 10% on activated carbon In ethyl acetate at 20℃; for 2h;	100%

2-methyl-4-nitrobenzoic acid (1975-51-5) → 4-amino-2-methylbenzoic acid (2486-75-1)

Conditions	Yield
With 5%-palladium/activated carbon; hydrogen In ethanol under 12001.2 Torr; Flow reactor;	98%
With hydrogenchloride; tin
With hydrogen; palladium 10% on activated carbon In methanol at 20℃; for 16h;

2-methyl-4-nitrobenzoic acid (1975-51-5) → (2-methyl-4-nitro-phenyl)methanol (22162-15-8)

Conditions	Yield
With Trimethyl borate; dimethylsulfide borane complex In tetrahydrofuran at 65℃; for 2h; Inert atmosphere;	98%
With Trimethyl borate; dimethylsulfide borane complex In tetrahydrofuran for 6h; Reduction; Heating;	93%
With Trimethyl borate; dimethylsulfide borane complex In tetrahydrofuran Reflux;	90%

2-methyl-4-nitrobenzoic acid (1975-51-5) + (S)-dibenzyl 2-(2-ethoxy-4-(5-((((R)-2-((R)-1-(N-hydroxyformamido)propyl)heptanamido)methyl)carbamoyl)furan-2-yl)benzamido)succinate → (S)-dibenzyl 2-(2-ethoxy-4-(5-((((R)-2-((R)-1-(N-((2-methyl-4-nitrobenzoyl)oxy)formamido)propyl)heptanamido)methyl)carbamoyl)furan-2-yl)benzamido)succinate

Conditions	Yield
With 4-methyl-morpholine; HATU In N,N-dimethyl-formamide; acetonitrile at 50℃; for 16h;	98%

2-methyl-4-nitrobenzoic acid (1975-51-5) → C8H4F3NO4

Conditions	Yield
With hydrogen fluoride; acetic acid; sodium nitrite In dichloromethane; water at 5 - 25℃; for 1h; Reagent/catalyst; Temperature;	95.8%

2-methyl-4-nitrobenzoic acid (1975-51-5) + 1-(2,3-dichlorophenyl)piperazine (41202-77-1) → (4-(2,3-dichlorophenyl)piperazin-1-yl)(2-methyl-4-nitrophenyl)methanone

Conditions	Yield
Stage #1: 2-methyl-4-nitrobenzoic acid With N-ethyl-N,N-diisopropylamine; HATU In N,N-dimethyl-formamide at 20℃; for 0.333333h; Stage #2: 1-(2,3-dichlorophenyl)piperazine In N,N-dimethyl-formamide at 20℃;	95%

isonipecotic acid methyl ester (2971-79-1) + 2-methyl-4-nitrobenzoic acid (1975-51-5) → methyl 1-(2-methyl-4-nitrobenzoyl)piperidine-4-carboxylate

Conditions	Yield
Stage #1: isonipecotic acid methyl ester; 2-methyl-4-nitrobenzoic acid With N-ethyl-N,N-diisopropylamine In dichloromethane at 20℃; for 0.5h; Inert atmosphere; Stage #2: With HATU In dichloromethane for 0h; Inert atmosphere;	93.4%
Stage #1: isonipecotic acid methyl ester; 2-methyl-4-nitrobenzoic acid With N-ethyl-N,N-diisopropylamine In dichloromethane at 20℃; for 0.5h; Stage #2: With N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate In dichloromethane	93.4%
Stage #1: isonipecotic acid methyl ester; 2-methyl-4-nitrobenzoic acid With N-ethyl-N,N-diisopropylamine In dichloromethane at 20℃; for 0.5h; Inert atmosphere; Stage #2: With N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate In dichloromethane for 10h; Inert atmosphere;	93.4%
Stage #1: isonipecotic acid methyl ester; 2-methyl-4-nitrobenzoic acid With N-ethyl-N,N-diisopropylamine In dichloromethane at 20℃; for 0.5h; Stage #2: With HATU In dichloromethane for 10h;	93.4%
Stage #1: isonipecotic acid methyl ester; 2-methyl-4-nitrobenzoic acid With N-ethyl-N,N-diisopropylamine In dichloromethane at 20℃; for 0.5h; Stage #2: With HATU In dichloromethane for 10h;	93.4%

2-methyl-4-nitrobenzoic acid (1975-51-5) + (E)-2-hydroxy-1-(methyl(oxo)(phenyl)-λ6-sulfaneylidene)guanidine → methyl((5-(2-methyl-4-nitrophenyl)-1,2,4-oxadiazol-3-yl)imino)(phenyl)-λ6-sulfanone

Conditions	Yield
With 2,4,6-tripropyl-1,3,5,2,4,6-trioxatriphosphinane-2,4,6-trioxide; N-ethyl-N,N-diisopropylamine In 2-methyltetrahydrofuran; ethyl acetate at 0 - 80℃; Inert atmosphere;	92%

2-methyl-4-nitrobenzoic acid (1975-51-5) → 2-methyl-4,5-dinitro-benzoic acid (101084-64-4)

Conditions	Yield
With sulfuric acid; nitric acid	89%
With sulfuric acid; nitric acid at 0 - 20℃; for 16h; Inert atmosphere;	89%
With sulfuric acid; nitric acid at 0 - 20℃; for 120h;	85%

ethanol (64-17-5) + 2-methyl-4-nitrobenzoic acid (1975-51-5) → 2-methyl-4-nitro-benzoic acid ethyl ester (62621-10-7)

Conditions	Yield
With sulfuric acid for 24h; Heating / reflux;	82.99%
sulfuric acid Reflux;

2-methyl-4-nitrobenzoic acid (1975-51-5) + 1-phenyl-propan-1-one (93-55-0) → C17H15NO5

Conditions	Yield
With 2,2,6,6-tetramethyl-piperidine-N-oxyl; chloro(1,5-cyclooctadiene)rhodium(I) dimer; copper diacetate; cesium fluoride In toluene at 120℃; for 24h; Inert atmosphere;	72%

2-methyl-4-nitrobenzoic acid (1975-51-5) → 1-methyl-3-nitrobenzene (99-08-1)

Conditions	Yield
With [Au(1,3-bis(2,6-diisopropylphenyl)-4,5-dihydroimidazol-2-ylidene)(O2CAd)] In toluene at 140℃; for 20h;	71%

2-methyl-4-nitrobenzoic acid (1975-51-5) + 4-amino-5-(naphthalen-1-yl-methyl)-3-mercapto-1,2,4-triazole (151297-83-5) → 3-(1-naphthylmethyl)-6-(2-nitro-4-methylphenyl)-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazole

Conditions	Yield
With trichlorophosphate for 4h; Heating;	65%

2-methyl-4-nitrobenzoic acid (1975-51-5) + 4-amino-5-[4-(N,N-dimethylamino)phenyl]-3-mercapto-1,2,4-triazole (76457-90-4) → 3-[4-(N,N-dimethylamino)phenyl]-6-(2-nitro-4-methylphenyl)-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazole

Conditions	Yield
With trichlorophosphate for 4h; Heating;	62%

4-amino-5-[2-(N-methylamino)phenyl]-3-mercapto-1,2,4-triazole (914978-98-6) + 2-methyl-4-nitrobenzoic acid (1975-51-5) → 3-[2-(N-methylamino)phenyl]-6-(2-nitro-4-methylphenyl)-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazole

Conditions	Yield
With trichlorophosphate for 4h; Heating;	60%

2-methyl-4-nitrobenzoic acid (1975-51-5) → 2-(bromomethyl)-4-nitrobenzoic acid (37156-27-7)

Conditions	Yield
With N-Bromosuccinimide; 2,2'-azobis(isobutyronitrile) In tetrachloromethane at 80℃; for 16h;	59%

Methylenbis(6-t-butyl-4-methyl-o-phenylen)hydrogenphosphit (15233-97-3) + 2-methyl-4-nitrobenzoic acid (1975-51-5) → C31H36NO6P

Conditions	Yield
Stage #1: 2-methyl-4-nitrobenzoic acid With thionyl chloride; N,N-dimethyl-formamide In dichloromethane at 20℃; for 6h; Inert atmosphere; Stage #2: Methylenbis(6-t-butyl-4-methyl-o-phenylen)hydrogenphosphit With N-ethyl-N,N-diisopropylamine In dichloromethane at 20℃; for 6h; Inert atmosphere;	55%

2-methyl-4-nitrobenzoic acid (1975-51-5) + tert-butyl methyl(3-(piperidine-4-carboxamido)propyl)carbamate → tert-butyl methyl(3-(1-(2-methyl-4-nitrobenzoyl)piperidine-4-carboxamido)propyl)carbamate

Conditions	Yield
With N-ethyl-N,N-diisopropylamine; HATU In N,N-dimethyl-formamide at 20℃; for 4h; Inert atmosphere;	47.16%
With N-ethyl-N,N-diisopropylamine; HATU In N,N-dimethyl-formamide at 20℃; for 4h;	47.16%
With N-ethyl-N,N-diisopropylamine; HATU In N,N-dimethyl-formamide at 20℃; for 4h;	47.16%
With N-ethyl-N,N-diisopropylamine; HATU In N,N-dimethyl-formamide at 20℃; for 4h;	47.16%

2-methyl-4-nitrobenzoic acid (1975-51-5) → 5-nitro-3H-isobenzofuran-1-one (67081-02-1)

Conditions	Yield
With sodium bromate; magnesium chloride In acetonitrile at 20℃; for 18h; Inert atmosphere; Irradiation; Sealed tube;	38%

2-methyl-4-nitrobenzoic acid (1975-51-5) → 2-methyl-4-nitrobenzoyl chloride (30459-70-2)

Conditions	Yield
With thionyl chloride
With thionyl chloride Heating;
With thionyl chloride Substitution;

2-methyl-4-nitrobenzoic acid (1975-51-5) + glycine ethyl ester hydrochloride (623-33-6) → (2-Methyl-4-nitro-benzoylamino)-acetic acid ethyl ester

Conditions	Yield
With 1,1'-carbonyldiimidazole 1) DMF, 0 deg C -> room temperature, 20 min, 2) DMF, room temperature, 30 min; Yield given. Multistep reaction;

Upstream product

• 99584-16-4 2-methyl-4-nitro-benzoic acid amide 
• 89001-53-6 2-cyano-5-nitrotoluene 
• 22162-16-9 2-methyl-4-nitrobenzylpyridinium bromide 
• 99-51-4 4-nitro-o-xylene 
• 7697-37-2 nitric acid 
• 116557-39-2 2-methyl-4-nitro-cinnamic acid 
• 2486-75-1 4-amino-2-methylbenzoic acid 
• 99-52-5 2-methyl-4-nitro-benzenamine 
• 6277-17-4 2-iodo-3-nitrotoluene 
• 108-88-3 toluene 
• 619-15-8 2,5-dinitrotoluene 
• 95-47-6 o-xylene 
• 7647-01-0 hydrogenchloride 
• 64-19-7 acetic acid 

Downstream Products

• 30459-70-2 2-methyl-4-nitrobenzoyl chloride 
• 2486-75-1 4-amino-2-methylbenzoic acid 
• 101084-64-4 2-methyl-4,5-dinitro-benzoic acid 
• 62621-09-4 methyl 2-methyl-4-nitrobenzoate 
• 22162-15-8 (2-methyl-4-nitro-phenyl)methanol 
• 914646-60-9 5-amino-2-benzylisoindolin-1-one 
• 914646-62-1 (E)-methyl 3-(2-benzyl-1-oxoisoindolin-5-yl)acrylate 
• 914646-63-2 (E)-3-(2-benzyl-1-oxoisoindolin-5-yl)acrylic acid 
• 914646-61-0 methyl 3-(2-benzyl-1-oxoisoindolin-5-yl)-2-bromopropanoate 
• 914646-64-3 (E)-3-(2-benzyl-1-oxoisoindolin-5-yl)-N-(tetrahydro-2H-pyran-2-yloxy)acrylamide 
• 133446-99-8 2-bromomethyl-4-nitro-benzoic acid methyl ester 
• 807343-00-6 2-benzyl-5-nitroisoindolin-1-one 
• 251643-27-3 Methyl 4-[N-methyl-N-(2-methyl-4-nitrobenzyloxycarbonyl)amino]phenylacetate 
• 251643-36-4 4-[N-Methyl-N-(2-methyl-4-nitrobenzyloxycarbonyl)amino]phenylacetic acid 

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An enantiomer, diastereoisomer or tautomer of a compound, represented by formula (I): wherein either A or B is nitrogen and the other B or A is C, and the radicals R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein, or a salt or ester thereof as viral polymerase inhibitors. The compound is used as an inhibitor of RNA dependent RNA polymerases, particularly those viral polymerases within the Flaviviridae family, more particularly to HCV polymerase.

DIARYL UREA DERIVATIVES IN THE TREATMENT OF PROTEIN KINASE DEPENDENT DISEASES

The invention relates to the use of diaryl urea derivatives for the manufacture of pharmaceutical compositions for the treatment of RET dependent disorders, especially RET dependent tumor diseases. The invention further relates to novel N-[4-(pyrimidin-4-yloxy)-phenyl]-N’-phenyl-urea derivatives and their use in the treatment of the animal or human body, especially in the treatment of a protein kinase dependent disease, to pharmaceutical compositions comprising such novel N-[4-pyrimidin-4-yloxy)-phenyl]-N’-phenyl-urea derivatives and to the use of such novel N-[4-(pyrimidin-4-yloxy)-phenyl]-N’-phenyl-urea derivatives for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as tumour diseases.