72235-52-0

Basic information

• Product Name: 2,4-Difluorobenzylamine
• Synonyms: 2,4-DIFLUOROBENZYLAMINE;RARECHEM AL BW 0282;2,4-Difluorobenzylamine 97%;2,4-Difluorobenzylamine97%;2,4-DIFLUOROBENZYLAMINE HYDROCHLORIDE;2,4-Difluorobenzylamine, 98+%;(2,4-Difluorophenyl)methanamine;Benzenemethanamine, 2,4-difluoro-
• CAS NO: 72235-52-0
• Molecular Formula: C₇H₇F₂N
• Molecular Weight: 143.13
• EINECS: 276-502-0
• Product Categories: Anilines, Aromatic Amines and Nitro Compounds;Amine;Amines;C7;Nitrogen Compounds
• Mol File: 72235-52-0.mol
• Article Data: 7

Chemical Properties

• Melting Point: 255-256 °C(Solv: N,N-dimethylformamide (68-12-2))
• Boiling Point: 82-84 °C (15 mmHg)
• Flash Point: 155 °F
• Appearance: Clear colorless to light yellow/Liquid
• Density: 1.204 g/mL at 25 °C(lit.)
• Vapor Pressure: 1.02mmHg at 25°C
• Refractive Index: n20/D 1.49(lit.)
• Storage Temp.: under inert gas (nitrogen or Argon) at 2–8 °C
• PKA: 8.58±0.10(Predicted)
• Sensitive: Air Sensitive
• BRN: 3539259
• CAS DataBase Reference: 2,4-Difluorobenzylamine(CAS DataBase Reference)
• NIST Chemistry Reference: 2,4-Difluorobenzylamine(72235-52-0)
• EPA Substance Registry System: 2,4-Difluorobenzylamine(72235-52-0)

Safety Data

• Hazard Codes: C
• Statements: 34
• Safety Statements: 26-27-36/37/39-45-25
• RIDADR: UN 2735 8/PG 3
• WGK Germany: 3
• HazardClass: 8
• PackingGroup: III
• Hazardous Substances Data: 72235-52-0(Hazardous Substances Data)

Usage

Chemical Properties

clear colorless to light yellow liquid

Uses

2,4-Difluorobenzylamine has been used in the synthesis of βAla–Aib(N-fluoroarylmethyl)], nonpolar nucleobase dipeptide via Ugi four-component condensation reaction.

InChI:InChI=1/C7H7F2N/c8-6-2-1-5(4-10)7(9)3-6/h1-3H,4,10H2/p+1

Synthetic route

C13H17F2N4(1+)*Br(1-) → 2,4-Difluoro-benzylamine (72235-52-0)

Conditions	Yield
With hydrogenchloride In methanol; water for 6h; Reflux;	90.8%

2,4-difluorobenzonitrile (3939-09-1) → 2,4-Difluoro-benzylamine (72235-52-0)

Conditions	Yield
With ammonium hydroxide; hydrogen In water; isopropyl alcohol at 60 - 80℃; under 7500.75 Torr; Temperature; Reagent/catalyst;	90%
With [ruthenium(II)(η6-1-methyl-4-isopropyl-benzene)(chloride)(μ-chloride)]2; 1,4-di(diphenylphosphino)-butane; iso-butanol; sodium hydroxide at 120℃; for 0.333333h; Inert atmosphere;	75 %Chromat.

1,3-Difluorobenzene (372-18-9) → 2,4-Difluoro-benzylamine (72235-52-0)

Conditions	Yield
Multi-step reaction with 3 steps 1: hydrogen bromide; iron(III) chloride / 1,4-dioxane / 7 h / Reflux 2: 1,4-dioxane / 4 h / Reflux 3: hydrogenchloride / water; methanol / 6 h / Reflux View Scheme
Multi-step reaction with 3 steps 1: hydrogenchloride; zinc(II) chloride / acetonitrile; water / 8 h / Reflux 2: toluene / 2 h / Reflux; Industrial scale 3: hydrogenchloride / water; isopropyl alcohol / 5 h / Reflux View Scheme
Multi-step reaction with 4 steps 1.1: nitrobenzene / 2 h / 70 - 105 °C 2.1: ozone / chlorobenzene / 1.5 h / 0 °C 3.1: thionyl chloride / dichloromethane / 1 h / 50 °C 3.2: 1.5 h / 50 °C 4.1: sodium chloride; bromine / 2 h / 50 °C View Scheme

2,4-difluorobenzyl chloride (452-07-3) → 2,4-Difluoro-benzylamine (72235-52-0)

Conditions	Yield
Multi-step reaction with 2 steps 1: toluene / 2 h / Reflux; Industrial scale 2: hydrogenchloride / water; isopropyl alcohol / 5 h / Reflux View Scheme

(2,4-difluoro-benzyl)-hexamethylenetetraminium; chloride → 2,4-Difluoro-benzylamine (72235-52-0)

Conditions	Yield
With hydrogenchloride In water; isopropyl alcohol for 5h; Reflux;

{1-benzyl-3-[(3-fluoro-4-nitro-benzenesulfonyl)-isobutyl-amino]-2-hydroxy-propyl}-carbamic acid hexahydro-furo[2,3-b]furan-3-yl ester (937397-44-9) + 2,4-Difluoro-benzylamine (72235-52-0) → (1-benzyl-3-{[3-(2,4-difluoro-benzylamino)-4-nitro-benzenesulfonyl]-isobutyl-amino}-2-hydroxy-propyl)-carbamic acid hexahydro-furo[2,3-b]furan-3-yl ester (937721-16-9)

Conditions	Yield
In tetrahydrofuran for 18h; Heating / reflux;	100%

2,4-Difluoro-benzylamine (72235-52-0) + acetyl chloride (75-36-5) → C9H9F2NO (1030596-28-1)

Conditions	Yield
With triethylamine at 20℃;	100%

2,4-Difluoro-benzylamine (72235-52-0) + methyl thioisocyanate (556-61-6) → 1-(2,4-difluorobenzyl)-3-methylthiourea (1400799-52-1)

Conditions	Yield
at 20℃;	99%

2,5-dimethyl 3-(benzyloxy)-1-(2,2-dimethoxyethyl)-4-oxo-1,4-dihydropyridine-2,5-dicarboxylate (1357289-08-7) + 2,4-Difluoro-benzylamine (72235-52-0) → 1-[2,2-bis(methyloxy)ethyl]-5-({[(2,4-difluorophenyl)methyl]amino}carbonyl)-4-oxo-3-[(phenylmethyl)oxy]-1,4-dihydro-2-pyridinecarboxylic acid methyl ester (1229006-21-6)

Conditions	Yield
With acetic acid In toluene at 90℃; for 7h; Reagent/catalyst;	97%
With acetic acid In toluene at 90 - 95℃; Solvent; regioselective reaction;	210 g

5-(((tert-butoxycarbonyl)amino)methyl)-2-(3-(cyclopropylmethoxy)-4-methoxyphenyl)oxazole-4-carboxylic acid + 2,4-Difluoro-benzylamine (72235-52-0) → tert-butyl ((2-(3-(cyclopropylmethoxy)-4-methoxyphenyl)-4-((2,4-difluorobenzyl)carbamoyl)oxazol-5-yl)methyl)carbamate

Conditions	Yield
Stage #1: 5-(((tert-butoxycarbonyl)amino)methyl)-2-(3-(cyclopropylmethoxy)-4-methoxyphenyl)oxazole-4-carboxylic acid With 1-hydroxy-7-aza-benzotriazole; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0℃; for 0.5h; Stage #2: 2,4-Difluoro-benzylamine With N-ethyl-N,N-diisopropylamine In dichloromethane at 0 - 20℃; for 12h;	97%

Octanoic acid (124-07-2) + 2,4-Difluoro-benzylamine (72235-52-0) → N-(2,4-difluorobenzyl)octanamide (816465-04-0)

Conditions	Yield
With 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; dmap In dichloromethane at 20℃;	96%

carbon monoxide (201230-82-2) + (3S,11 aR)-8-bromo-3-methyl-6-[(phenyl-methyl)oxy]-2,3,11,11a-tetrahydro[1,3]oxazolo[3,2-a] pyrido[1,2-d]pyrazine-5,7-dione (1206103-44-7) + 2,4-Difluoro-benzylamine (72235-52-0) → (3S,11aR)-N-[(2,4-difluorophenyl)methyl]-3-methyl-5,7-dioxo-6-[(phenylmethyl)oxy]-2,3,5,7,11,11a-hexahydro[1,3]oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide (1206103-45-8)

Conditions	Yield
With N-ethyl-N,N-diisopropylamine; tetrakis(triphenylphosphine) palladium(0) In dimethyl sulfoxide at 90℃; for 9h;	96%
With tetrakis(triphenylphosphine) palladium(0); N-ethyl-N,N-diisopropylamine In dimethyl sulfoxide at 90℃; for 9h;	96%
With tetrakis(triphenylphosphine) palladium(0); N-ethyl-N,N-diisopropylamine In dimethyl sulfoxide at 90℃; for 7h;	96%

1-(2,2-dimethoxy-ethyl)-3-methoxy-4-oxo-1,4-dihydro-pyridine-2,5-dicarboxylic acid dimethyl ester + 2,4-Difluoro-benzylamine (72235-52-0) → methyl 5-((2,4-difluorobenzyl)carbamoyl)-1-(2,2-dirnethoxyethyl)-3-methoxy-4-oxo-1,4-dihydropyridine-2-carboxylate (1616340-68-1)

Conditions	Yield
With acetic acid In toluene at 200℃; under 5171.62 Torr; Solvent; Reagent/catalyst; Temperature; Flow reactor; chemoselective reaction;	96%

benzothiazole-2-carboxylic acid ethyl ester (32137-76-1) + 2,4-Difluoro-benzylamine (72235-52-0) → N-(2,4-difluorobenzyl)benzo[d]thiazole-2-carboxamide

Conditions	Yield
In acetonitrile at 100℃; for 0.25h; Sealed tube; Microwave irradiation;	95%

C8H14O5 + 2,4-Difluoro-benzylamine (72235-52-0) → C15H19F2NO4

Conditions	Yield
Stage #1: C8H14O5 With 4-methyl-morpholine; chloroformic acid ethyl ester In tetrahydrofuran at 0 - 15℃; for 0.5h; Stage #2: 2,4-Difluoro-benzylamine In tetrahydrofuran at 0 - 20℃; for 1h; Reagent/catalyst; Solvent;	95%
Stage #1: C8H14O5 With 4-methyl-morpholine; chloroformic acid ethyl ester In tetrahydrofuran at 0 - 30℃; for 0.5h; Stage #2: 2,4-Difluoro-benzylamine In tetrahydrofuran at 10 - 15℃; for 1h;	94%

N-(2,4-difluorobenzyl)-N-(4-ethylbenzyl)amine (816465-13-1) + 2,4-Difluoro-benzylamine (72235-52-0) → N-(2,4-difluorobenzyl)-4-ethylbenzamide

Conditions	Yield
With 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; dmap In dichloromethane at 20℃;	94%

(S)-5-(1-((tert-butoxycarbonyl)amino)-2-phenylethyl)-2-(3-(cyclopropylmethoxy)-4-methoxyphenyl)oxazole-4-carboxylic acid + 2,4-Difluoro-benzylamine (72235-52-0) → (S)-tert-butyl (1-(2-(3-(cyclopropylmethoxy)-4-methoxyphenyl)-4-((2,4-difluorobenzyl)carbamoyl)oxazol-5-yl)-2-phenylethyl)carbamate

Conditions	Yield
Stage #1: (S)-5-(1-((tert-butoxycarbonyl)amino)-2-phenylethyl)-2-(3-(cyclopropylmethoxy)-4-methoxyphenyl)oxazole-4-carboxylic acid With 1-hydroxy-7-aza-benzotriazole; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 20℃; for 0.5h; Stage #2: 2,4-Difluoro-benzylamine With N-ethyl-N,N-diisopropylamine In dichloromethane at 20℃; for 12h;	94%

carbon disulfide (75-15-0) + 2,4-Difluoro-benzylamine (72235-52-0) + ethylene dibromide (106-93-4) → 3-(2,4-difluorobenzyl)thiazolidine-2-thione

Conditions	Yield
Stage #1: carbon disulfide; 2,4-Difluoro-benzylamine With N-benzyl-trimethylammonium hydroxide In dimethyl sulfoxide at 20℃; for 0.25h; Green chemistry; Stage #2: ethylene dibromide In dimethyl sulfoxide at 20℃; Inert atmosphere; Green chemistry;	93.95%

(4R,12aS)-3,4,6,8,12,12a-hexahydro-4-methyl-6,8-dioxo-7-(phenylmethoxy)-2H-pyrido [1',2':4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxylic acid (1339879-91-2) + 2,4-Difluoro-benzylamine (72235-52-0) → (4R,12aS)-7-(benzyloxy)-N-(2,4-difluorobenzyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1′,2’:4,5]-pyrazino[2,1-b][1,3]oxazine-9-carboxamide (1206102-11-5)

Conditions	Yield
With 1,1'-carbonyldiimidazole In dichloromethane for 36h;	93.3%
With 4-methyl-morpholine; HATU In N,N-dimethyl-formamide at 20℃; for 32h;	73%

2,4-Difluoro-benzylamine (72235-52-0) + 2-amino-6-chloro-3-nitropyridine (27048-04-0) → N2-(2,4-difluorobenzyl)-5-nitropyridine-2,6-diamine (157840-46-5)

Conditions	Yield
With triethylamine In isopropyl alcohol for 3h; Reflux; Inert atmosphere;	93%
With triethylamine In 1,4-dioxane

5-bromouracil (51-20-7) + 2,4-Difluoro-benzylamine (72235-52-0) → 5-[(2,4-difluorobenzyl)amino]dihydropyrimidine-2,4(1H,3H)-dione (867151-48-2)

Conditions	Yield
at 160℃; for 6h;	93%
at 160℃; for 2h;	91%

nonanoic acid (112-05-0) + 2,4-Difluoro-benzylamine (72235-52-0) → N-(2,4-difluorobenzyl)nonanamide (816465-08-4)

Conditions	Yield
With 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; dmap In dichloromethane at 20℃;	93%

(S)-5-(1-((tert-butoxycarbonyl)amino)-2-methylpropyl)-2-(3-(cyclopropylmethoxy)-4-methoxyphenyl)oxazole-4-carboxylic acid + 2,4-Difluoro-benzylamine (72235-52-0) → (S)-tert-butyl (1-(2-(3-(cyclopropylmethoxy)-4-methoxyphenyl)-4-((2,4-difluorobenzyl)carbamoyl)oxazol-5-yl)-2-methylpropyl)carbamate

Conditions	Yield
Stage #1: (S)-5-(1-((tert-butoxycarbonyl)amino)-2-methylpropyl)-2-(3-(cyclopropylmethoxy)-4-methoxyphenyl)oxazole-4-carboxylic acid With 1-hydroxy-7-aza-benzotriazole; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 20℃; for 0.5h; Stage #2: 2,4-Difluoro-benzylamine With N-ethyl-N,N-diisopropylamine In dichloromethane at 0 - 20℃; for 12h;	93%

10H-phenothiazine-10-carbonyl chloride (18956-87-1) + 2,4-Difluoro-benzylamine (72235-52-0) → N-(2,4-difluorobenzyl)-10H-phenothiazine-10-carboxamide

Conditions	Yield
With triethylamine In dichloromethane at 20℃; for 1h;	92.8%

3-isobutyl-1-(thiazol-2-yl)-1H-pyrazole-4-carboxylic acid + 2,4-Difluoro-benzylamine (72235-52-0) → N-(2,4-difluorobenzyl)-3-isobutyl-1-(thiazol-2-yl)-1H-pyrazole-4-carboxamide

Conditions	Yield
Stage #1: 3-isobutyl-1-(thiazol-2-yl)-1H-pyrazole-4-carboxylic acid With HATU In N,N-dimethyl-formamide for 0.166667h; Stage #2: 2,4-Difluoro-benzylamine With triethylamine In N,N-dimethyl-formamide at 20℃; for 1h;	92%

Phenyl glycidyl ether (122-60-1) + 2,4-Difluoro-benzylamine (72235-52-0) → 1-[(2,4-difluorobenzyl)amino]-3-phenoxypropan-2-ol

Conditions	Yield
Stage #1: Phenyl glycidyl ether; 2,4-Difluoro-benzylamine In N,N-dimethyl-formamide at 60℃; for 12h; Sealed tube; Stage #2: With water In N,N-dimethyl-formamide at 60℃; for 12h; Sealed tube; regioselective reaction;	92%

4-oxo-piperidine-1-carboxylic acid 2-(trimethylsilyl)ethyl ester (181701-30-4) + 2,4-Difluoro-benzylamine (72235-52-0) → 2-(trimethylsilyl)ethyl 4-{[(2,4-difluorophenyl)methyl]amino}piperidine-1-carboxylate

Conditions	Yield
With ethanol; sodium tris(acetoxy)borohydride for 22h;	92%
With sodium tris(acetoxy)borohydride In dichloromethane at 20℃; for 1h;	3.49 g

2,4-Difluoro-benzylamine (72235-52-0) + 1,1-di(methylsulfanyl)-2-nitroethylene (13623-94-4) → N,N'-bis(2,4-difluorobenzyl)-2-nitroethylene-1,1-diamine

Conditions	Yield
In ethanol for 12h; Reflux;	91%

1-Methyl-4-piperidone (1445-73-4) + 2,4-Difluoro-benzylamine (72235-52-0) → N-[(2,4-difluorophenyl)methyl]-1-methylpiperidin-4-amine

Conditions	Yield
With ethanol; sodium tris(acetoxy)borohydride at 20℃; for 2h;	91%
With ethanol; sodium tris(acetoxy)borohydride at 20℃; for 2h;	91%

carbon monoxide (201230-82-2) + (4R,12aS)-7-(benzyloxy)-9-bromo-4-methyl-3,4,12,12atetrahydro-2H-pyrido [1′,2′:4,5]pyrazino[2,1-b][1,3]oxazine-6,8-dione (1206102-10-4) + 2,4-Difluoro-benzylamine (72235-52-0) → (4R,12aS)-7-(benzyloxy)-N-(2,4-difluorobenzyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1′,2’:4,5]-pyrazino[2,1-b][1,3]oxazine-9-carboxamide (1206102-11-5)

Conditions	Yield
With tetrakis(triphenylphosphine) palladium(0) In dimethyl sulfoxide at 90℃; for 5h; Large scale;	90%
With N-ethyl-N,N-diisopropylamine; tetrakis(triphenylphosphine) palladium(0) In dimethyl sulfoxide at 90℃; for 5.5h; Product distribution / selectivity;	84%
With tetrakis(triphenylphosphine) palladium(0); N-ethyl-N,N-diisopropylamine In dimethyl sulfoxide at 90℃; for 5.5h; Solvent;	84%
With tetrakis(triphenylphosphine) palladium(0)

methyl 1-(benzyloxy)-4-hydroxy-2-oxo-7-(piperidin-1-yl)-1,2-dihydro-1,8-naphthyridine-3-carboxylate + 2,4-Difluoro-benzylamine (72235-52-0) → 1-(benzyloxy)-N-(2,4-difluorobenzyl)-4-hydroxy-2-oxo-7-(piperidin-1-yl)-1,2-dihydro-1,8-naphthyridine-3-carboxamide

Conditions	Yield
In N,N-dimethyl-formamide at 140℃; for 2h; Microwave irradiation;	90%

N-[5-(4-fluoro-3-nitrophenyl)-[1,3,4]thiadiazol-2-yl]-2,2-dimethylpropionamide + 2,4-Difluoro-benzylamine (72235-52-0) → N-{5-[4-(2,4-difluorobenzylamino)-3-nitrophenyl]-[1,3,4]thiadiazol-2-yl}-2,2-dimethylpropionamide

Conditions	Yield
In ethanol at 100℃; for 1h; Microwave irradiation;	89%

2-(4-fluoro-3-nitrophenyl)-5-(4-methoxyphenyl)imidazo[2,1-b][1,3,4]thiadiazole + 2,4-Difluoro-benzylamine (72235-52-0) → (2,4-difluorobenzyl)-{4-[5-(4-methoxyphenyl)imidazo[2,1-b][1,3,4]thiadiazol-2-yl]-2-nitrophenyl}amine

Conditions	Yield
In ethanol at 100℃; for 1h; Microwave irradiation;	89%

Upstream product

• 3939-09-1 2,4-difluorobenzonitrile 
• 372-18-9 1,3-Difluorobenzene 
• 452-07-3 2,4-difluorobenzyl chloride 
• 81228-02-6 2-(2,4-difluorophenyl)ethanol 
• 399-34-8 2-(2,4-difluorophenyl)acetamide 
• 729559-69-7 N-(4-cyanophenyl)-2,4-difluorobenzamide 
• 72482-64-5 2,4-difluorobenzoyl chloride 
• 1583-58-0 2,4-difluoro-benzoic acid 
• 13656-36-5 3,5-dichloro-2,4,6-trifluorobenzoic acid 

Downstream Products

• 329314-71-8 N-(tert-butoxycarbonyl-β-alanyl)-N-(2,4-difluorobenzyl)-2-methylalanine (N-cyclohex-1-enyl) amide 
• 1027896-08-7 (7-chloro-6-nitro-quinazolin-4-yl)-(2,4-difluoro-benzyl)-amine 
• 348134-45-2 9-(4-bromo-butyl)-9H-fluorene-9-carboxylic acid-2,4-difluoro-benzylamide 
• 134672-66-5 1-[(2,4-Difluorophenyl)methyl]-2,5-dimethyl-1H-pyrrole 
• 330669-95-9 (R)-1-(2,4-difluoro-benzylamino)-3-[4-(6-fluoro-benzo[d]isoxazol-3-yl)-phenoxy]-propan-2-ol 
• 1080433-45-9 1-(2',4'-difluorobenzyl)-5-nitrouracil 
• 1019853-69-0 C₃₃H₂₅F₂N₅O 
• 1181328-49-3 C₂₉H₂₂F₂N₂ 
• 1181328-59-5 C₂₉H₂₁F₃N₂ 
• 1183806-92-9 4-{[(2,4-difluorobenzyl)amino]methyl}benzonitrile 
• 1201816-89-8 (E)-1-(2,4-difluorobenzyl)-5-((2,4-difluorobenzylimino)(2-hydroxy-4-methoxyphenyl)methyl)pyridin-2(1H)-one 
• 1201219-03-5 perfluorophenyl 4-(4-(4-(5-(2,5-difluorobenzylcarbamoyl)-1-methyl-1H-pyrrol-3-ylcarbamoyl)benzoyl)benzamido)-1-methyl-1H-pyrrole-2-carboxylate 

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