2927-71-1

Basic information

• Product Name: 2,4-Dichloro-5-fluoropyrimidine
• Synonyms: CHEMPACIFIC 37950;5-FLUORO-2,4-DICHLOROPYRIMIDINE;2,4-DICHLORO-5-FLUOROPYRIMIDINE;2,4-Dichloro-5-fluorouracil;5-Fluoro-2,4-dichloropyrimdine;2,6-DICHLORO-5-FLUORORACIL;2,4-Dichloro-5-Fluoropyrimidin;2,4-Dichloro-5-fluoropyrimidine99%
• CAS NO: 2927-71-1
• Molecular Formula: C₄HCl₂FN₂
• Molecular Weight: 166.97
• EINECS: 249-616-3
• Product Categories: Pyrimidine Series;Heterocycles;Pyridines, Pyrimidines, Purines and Pteredines;pharmacetical;Halides;Pyrazines, Pyrimidines & Pyridazines;Pyrimidine;Building Blocks;Fluorinated;Nucleotides and Nucleosides;Bases & Related Reagents;Nucleotides;Pyrazines, Pyrimidines & Pyridazines;Building Blocks;Halogenated Heterocycles;Heterocyclic Building Blocks;Pyrimidines;PyrimidinesHeterocyclic Building Blocks;Aromatics;Fluorine series
• Mol File: 2927-71-1.mol

Chemical Properties

• Melting Point: 37-41 °C(lit.)
• Boiling Point: 80 °C / 16mmHg
• Flash Point: 223 °F
• Appearance: White to pale brown/Powder or Crystalline Powder or Low Melting Solid
• Density: 1.605 g/cm³
• Vapor Pressure: 0.148mmHg at 25°C
• Refractive Index: 1.531
• Storage Temp.: -20°C Freezer, Under Inert Atmosphere
• PKA: -3.96±0.29(Predicted)
• Sensitive: Moisture Sensitive
• CAS DataBase Reference: 2,4-Dichloro-5-fluoropyrimidine(CAS DataBase Reference)
• NIST Chemistry Reference: 2,4-Dichloro-5-fluoropyrimidine(2927-71-1)
• EPA Substance Registry System: 2,4-Dichloro-5-fluoropyrimidine(2927-71-1)

Safety Data

• Hazard Codes: Xi,C
• Statements: 36/37/38-34-22
• Safety Statements: 26-36-37/39-45-36/37/39
• RIDADR: 3261
• WGK Germany: 3
• HazardClass: IRRITANT
• PackingGroup: Ⅲ
• Hazardous Substances Data: 2927-71-1(Hazardous Substances Data)

Usage

Uses

Used in Pharmaceutical Industry:
2,4-Dichloro-5-fluoropyrimidine is used as a key intermediate for the synthesis of glucuronic derivatives of 5-fluorouracil, which are neoplasm inhibitors. These derivatives have potential applications in cancer treatment, as they can help inhibit the growth of tumors.
2,4-Dichloro-5-fluoropyrimidine is also used as a starting material for the synthesis of various potential kinase inhibitors, including 5-fluoropyrimidine-2-carboxamides, 5-fluoropyrimidine-4-carboxamides, a series of 2,4-diamino-5-fluoropyrimidine derivatives, and 2,4-bisanilinopyrimidine derivatives. These compounds have potential applications in the development of targeted cancer therapies, as they can inhibit specific enzymes involved in cancer cell proliferation and survival.
Furthermore, 2,4-dichloro-5-fluoropyrimidine is used in the synthesis of 5-fluoro-N,N-bis(4-methoxyphenyl)-2,4-pyrimidinediamine and 2-chloro-5-fluoro-4-(4-fluorophenyl)pyrimidine, which are important intermediates in the development of novel anticancer agents. The former is synthesized by reacting p-methoxy aniline in the presence of DIPEA, while the latter is obtained through a Suzuki coupling reaction using (4-fluorophenyl)boronic acid, triphenylphosphine, and a palladium(II) acetate catalyst.
Additionally, 2,4-dichloro-5-fluoropyrimidine is used in the preparation of 5-fluoro-2-(piperidin-4-yloxy)pyrimidin-4-amine, a scaffold that is employed in the development of potent deoxycytidine kinase inhibitors. These inhibitors have potential applications in the treatment of various types of cancer, as they can disrupt the DNA synthesis and repair mechanisms in cancer cells, leading to cell death.

Flammability and Explosibility

Notclassified

InChI:InChI=1/C4HCl2FN2/c5-3-2(7)1-8-4(6)9-3/h1H

Synthetic route

2,4-dimethoxy-5-fluoropyrimidine (4330-22-7) → 2,4-dichloro-5-fluoropyrimidine (2927-71-1)

Conditions	Yield
Stage #1: 5-fluoro-2,4-dimethoxypyrimidine With thionyl chloride In chloroform at 0℃; for 0.5h; UV-irradiation; Stage #2: With chlorine In chloroform at 20℃; for 12h; Solvent; Wavelength; UV-irradiation;	98%

5-fluoropyrimidine-2,4-diol (51-21-8) → 2,4-dichloro-5-fluoropyrimidine (2927-71-1)

Conditions	Yield
With trichlorophosphate In N,N-dimethyl-aniline at 100℃; for 13h; Inert atmosphere; Large scale;	95%
With pyridine; trichlorophosphate at 180℃; under 150.015 - 900.09 Torr; for 2h; Neat (no solvent);	93%
With dimethyl amine; trichlorophosphate at 95 - 120℃; for 4h;	92%

5-fluorouracil (51-21-8) → 2,4-dichloro-5-fluoropyrimidine (2927-71-1)

Conditions	Yield
With dimethyl amine; trichlorophosphate at 95 - 120℃; for 4h;	94%
With phosphorus pentachloride for 4h; Heating;	91%
Stage #1: 5-fluorouracil With trichlorophosphate at 95℃; for 3.5h; Stage #2: With hydrogenchloride In water at 0 - 20℃;	87%

2,4,6-trichloro-5-fluoropyrimidine (6693-08-9) → 2,4-dichloro-5-fluoropyrimidine (2927-71-1)

Conditions	Yield
With hydrogen; triethylamine; palladium on activated charcoal In ethyl acetate at 30℃; under 2625.2 Torr;	87%

ethyl bromide (74-96-4) → 2,4-dichloro-5-fluoropyrimidine (2927-71-1)

Conditions	Yield
With magnesium In tetrahydrofuran

morpholine (110-91-8) + 2,4-dichloro-5-fluoropyrimidine (2927-71-1) → 4-(2-chloro-5-fluoro-pyrimidin-4-yl)morpholine (31646-53-4)

Conditions	Yield
In water at 60 - 70℃; for 2.5h;	100%
With N-ethyl-N,N-diisopropylamine In ethanol Reflux; regioselective reaction;	95%
With N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide for 1h; Inert atmosphere; Reflux;	85%

piperidine (110-89-4) + 2,4-dichloro-5-fluoropyrimidine (2927-71-1) → 2-chloro-5-fluoro-4-piperidin-1-yl-pyrimidine (40423-82-3)

Conditions	Yield
In water at 60 - 70℃; for 2.5h;	100%

1-n-propylpiperazine (21867-64-1) + 2,4-dichloro-5-fluoropyrimidine (2927-71-1) → 2-Chloro-5-fluoro-4-(4-propyl-piperazin-1-yl)-pyrimidine

Conditions	Yield
In water at 60 - 70℃; for 2.5h;	100%

2,4-dichloro-5-fluoropyrimidine (2927-71-1) → 2-chloro-5-fluoropyrimidin-4-amine (155-10-2)

Conditions	Yield
With ammonium hydroxide at 60 - 70℃; for 2.5h;	100%
With ammonia In water Substitution;
With ammonium hydroxide In ethanol at 25 - 35℃; for 3.5h;

(R)-tert-butyl (1-aminobutan-2-yl)carbamate (956125-05-6) + 2,4-dichloro-5-fluoropyrimidine (2927-71-1) → {(R)-1-[(2-Chloro-5-fluoro-pyrimidin-4-ylamino)-methyl]-propyl}-carbamic acid tert-butyl ester (956125-24-9)

Conditions	Yield
With triethylamine In acetonitrile at 0℃; for 3h;	100%

4-methoxy-aniline (104-94-9) + 2,4-dichloro-5-fluoropyrimidine (2927-71-1) → 5-fluoro-N2,N4-bis(4-methoxyphenyl)pyrimidine-2,4-diamine diformate

Conditions	Yield
Stage #1: 4-methoxy-aniline; 2,4-dichloro-5-fluoropyrimidine With N-ethyl-N,N-diisopropylamine In 1,4-dioxane at 160℃; for 0.333333h; Microwave irradiation; Stage #2: With formic acid In water; acetonitrile	100%

4-fluoroboronic acid (1765-93-1) + 2,4-dichloro-5-fluoropyrimidine (2927-71-1) → 2-chloro-5-fluoro-4-(4-fluorophenyl)pyrimidine (1341200-71-2)

Conditions	Yield
With palladium diacetate; sodium carbonate; triphenylphosphine In tetrahydrofuran; water for 12h; Suzuki coupling; Reflux;	100%

(S)-1-(1-methyl-6-(1-methyl-1H-pyrazol-5-yl)-1H-pyrrolo[3,2-b]pyridin-5-yl)ethanamine (1537256-09-9) + 2,4-dichloro-5-fluoropyrimidine (2927-71-1) → (S)-2-chloro-5-fluoro-N-(1-(1-methyl-6-(1-methyl-1H-pyrazol-5-yl)-1H-pyrrolo[3,2-b]pyridin-5-yl)ethyl)pyrimidin-4-amine (1537207-28-5)

Conditions	Yield
With N-ethyl-N,N-diisopropylamine In acetonitrile at 120℃; for 1h; Microwave irradiation;	100%

n-propylmagnesium bromide (927-77-5) + 2,4-dichloro-5-fluoropyrimidine (2927-71-1) → 2,4-dichloro-5-fluoro-6-propylpyrimidine

Conditions	Yield
Stage #1: n-propylmagnesium bromide; 2,4-dichloro-5-fluoropyrimidine In tetrahydrofuran; 1,2-dimethoxyethane at 15℃; for 1h; Stage #2: With iodine; triethylamine In tetrahydrofuran; 1,2-dimethoxyethane at 5℃;	100%

cyclopropanol (16545-68-9) + 2,4-dichloro-5-fluoropyrimidine (2927-71-1) → 2-chloro-4-cyclopropoxy-5-fluoropyrimidine

Conditions	Yield
Stage #1: cyclopropanol With sodium hydride In tetrahydrofuran; mineral oil at 0℃; for 0.333333h; Stage #2: 2,4-dichloro-5-fluoropyrimidine In tetrahydrofuran; mineral oil at 0℃; for 4h;	100%

2,4-dichloro-5-fluoropyrimidine (2927-71-1) + 4-fluoroaniline (371-40-4) → 2-chloro-5-fluoro-N-(4-fluorophenyl)pyrimidin-4-amine (1049666-34-3)

Conditions	Yield
With trifluoroacetic acid In ethanol at 20℃; for 24h; regioselective reaction;	99%
In methanol; water at 50℃; for 5h;	68%
With N-ethyl-N,N-diisopropylamine In butan-1-ol at 80℃; for 1.5h;

Nα-isobutyl-Nβ-Boc-hydrazine (57699-53-3) + 2,4-dichloro-5-fluoropyrimidine (2927-71-1) → C13H20ClFN4O2 (929016-08-0)

Conditions	Yield
With N-ethyl-N,N-diisopropylamine In isopropyl alcohol Reflux;	99%

7-fluoro-2,3,3-trimethyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-3H-indole + 2,4-dichloro-5-fluoropyrimidine (2927-71-1) → 5-(2-chloro-5-fluoropyrimidin-4-yl)-7-fluoro-2,3,3-trimethyl-3H-indole

Conditions	Yield
With potassium phosphate; tetrakis(triphenylphosphine) palladium(0) In 1,4-dioxane; water at 130℃; for 1h; Suzuki Coupling; Inert atmosphere; Microwave irradiation;	99%
With tetrakis(triphenylphosphine) palladium(0) In 1,4-dioxane; water at 130℃; for 1h; Microwave irradiation; Inert atmosphere;	301.2 mg

2-pyridylmethyl 4-tolyl sulfone (58414-96-3) + 2,4-dichloro-5-fluoropyrimidine (2927-71-1) → 2-Chloro-10-(toluene-4-sulfonyl)-pyrimido[4,5-b]indolizine (137890-00-7)

Conditions	Yield
With potassium carbonate In N,N-dimethyl-formamide Heating;	98%

2,4-dichloro-5-fluoropyrimidine (2927-71-1) + Diethyl methylmalonate (609-08-5) → 2-methyl-2-(2-chloro-5-fluoropyrimidinyl-4-yl)-1,3-propanedioic acid diethyl ester (137234-89-0)

Conditions	Yield
Stage #1: Diethyl methylmalonate With sodium hydride In tetrahydrofuran; mineral oil at -10℃; for 0.5h; Stage #2: 2,4-dichloro-5-fluoropyrimidine In tetrahydrofuran; mineral oil at -10℃; for 0.5h;	98%
With sodium hydride In tetrahydrofuran; mineral oil at -10℃; for 0.5h;	83%

1-(4-{4-amino-3-methoxyphenyl}piperazine-1-yl)ethan-1-one (1021426-42-5) + 2,4-dichloro-5-fluoropyrimidine (2927-71-1) → 1-(4-(4-((2-chloro-5-fluoropyrimidin-4-yl)amino)-3-methoxyphenyl)piperazin-1-yl)ethanone (1474014-16-8)

Conditions	Yield
With potassium carbonate In N,N-dimethyl-formamide at 50℃; Temperature;	98%
With potassium carbonate In N,N-dimethyl-formamide at 80℃;	68%

2,4-dichloro-5-fluoropyrimidine (2927-71-1) + 1-methyl-5-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-1H-pyrazole (847818-74-0) → 2-chloro-5-fluoro-4-(1-methyl-1H-pyrazol-5-yl)pyrimidine

Conditions	Yield
With (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride; sodium carbonate In tetrahydrofuran; water Reflux;	98%

N-(1,3-benzodioxol-5-ylmethyl)-2-(tetrahydro-2H-pyran-4-yl)ethanamine + 2,4-dichloro-5-fluoropyrimidine (2927-71-1) → N-(1,3-benzodioxol-5-ylmethyl)-2-chloro-5-fluoro-N-[2-(tetrahydro-2H-pyran-4-yl)ethyl]pyrimidin-4-amine

Conditions	Yield
With N-ethyl-N,N-diisopropylamine In isopropyl alcohol at 85℃;	98%

methyl 6-azaspiro[2.5]octane-1-carboxylate hydrochloride + 2,4-dichloro-5-fluoropyrimidine (2927-71-1) → methyl 6-(2-chloro-5-fluoropyrimidin-4-yl)-6-azaspiro[2.5]octane-1-carboxylate

Conditions	Yield
With triethylamine In methanol at 30℃; for 16h;	98%

3-methyl-5-aminopyrazole (31230-17-8) + 2,4-dichloro-5-fluoropyrimidine (2927-71-1) → 2-chloro-5-fluoro-N-(5-methyl-1H-pyrazol-3-yl)pyrimidin-4-amine (851434-99-6)

Conditions	Yield
With triethylamine In ethanol at 0 - 25℃; regioselective reaction;	97%
With N-ethyl-N,N-diisopropylamine In ethanol at 20℃; for 48h; Inert atmosphere;	86%
With N-ethyl-N,N-diisopropylamine In ethanol at 20℃; for 48h; Inert atmosphere;	86%
With triethylamine In ethanol at 18 - 25℃; for 12h;
With triethylamine In ethanol at 18 - 25℃; for 12h;

2-fluorobenzylamine (89-99-6) + 2,4-dichloro-5-fluoropyrimidine (2927-71-1) → (2-chloro-5-fluoropyrimidin-4-yl)-(2-fluorobenzyl)amine (1174385-80-8)

Conditions	Yield
With triethylamine In tetrahydrofuran for 5h; Reflux;	97%
With triethylamine In tetrahydrofuran at 80℃; for 5h;	97%

N-(1,3-benzodioxol-5-ylmethyl)-3-(5-phenyl-1,2,4-oxadiazol-3-yl)propan-1-amine + 2,4-dichloro-5-fluoropyrimidine (2927-71-1) → N-(1,3-benzodioxol-5-ylmethyl)-2-chloro-5-fluoro-N-[3-(5-phenyl-1,2,4-oxadiazol-3-yl)propyl]pyrimidin-4-amine

Conditions	Yield
With N-ethyl-N,N-diisopropylamine In isopropyl alcohol at 85℃;	97%

tert-butyl 3-hydroxyphenylcarbamate (19962-06-2) + 2,4-dichloro-5-fluoropyrimidine (2927-71-1) → C15H15ClFN3O3 (1246610-46-7)

Conditions	Yield
With N-ethyl-N,N-diisopropylamine In butan-1-ol at 110℃; for 16h;	96%

2,4-dichloro-5-fluoropyrimidine (2927-71-1) + sodium thiomethoxide (5188-07-8) → 2-chloro-5-fluoro-4-methylthiopyrimidine

Conditions	Yield
In tetrahydrofuran at -30℃; for 2h;	96%
In tetrahydrofuran; water at -30℃; for 2h;	93%
In tetrahydrofuran at 20℃; for 12h;

N-(1,3-benzodioxol-5-ylmethyl)-1-methylcyclopropanamine + 2,4-dichloro-5-fluoropyrimidine (2927-71-1) → N-(1,3-benzodioxol-5-ylmethyl)-2-chloro-5-fluoro-N-(1-methylcyclopropyl)pyrimidin-4-amine

Conditions	Yield
With N-ethyl-N,N-diisopropylamine In isopropyl alcohol at 85℃;	96%

N-(1,3-benzodioxol-5-ylmethyl)-2-(4-fluorophenyl)ethanamine + 2,4-dichloro-5-fluoropyrimidine (2927-71-1) → N-(1,3-benzodioxol-5-ylmethyl)-2-chloro-5-fluoro-N-[2-(4-fluorophenyl)ethyl]pyrimidin-4-amine

Conditions	Yield
With N-ethyl-N,N-diisopropylamine In isopropyl alcohol at 85℃;	96%

1-(1,3-benzodioxol-5-yl)-N-(cyclopropylmethyl)methanamine + 2,4-dichloro-5-fluoropyrimidine (2927-71-1) → N-(1,3-benzodioxol-5-ylmethyl)-2-chloro-N-(cyclopropylmethyl)-5-fluoropyrimidin-4-amine

Conditions	Yield
With N-ethyl-N,N-diisopropylamine In ethanol; isopropyl alcohol at 85℃;	96%

N-(1,3-benzodioxol-5-ylmethyl)-2-(4-chloro-3,5-dimethylphenoxy)ethanamine + 2,4-dichloro-5-fluoropyrimidine (2927-71-1) → N-(1,3-benzodioxol-5-ylmethyl)-2-chloro-N-[2-(4-chloro-3,5-dimethylphenoxy)ethyl]-5-fluoropyrimidin-4-amine

Conditions	Yield
With N-ethyl-N,N-diisopropylamine In isopropyl alcohol at 85℃;	96%

Upstream product

• 51-21-8 5-fluorouracil 
• 51-21-8 5-fluoropyrimidine-2,4-diol 
• 6693-08-9 2,4,6-trichloro-5-fluoropyrimidine 
• 74-96-4 ethyl bromide 
• 4330-22-7 5-fluoro-2,4-dimethoxypyrimidine 

Downstream Products

• 31646-53-4 4-(2-chloro-5-fluoro-pyrimidin-4-yl)morpholine 
• 40423-82-3 2-chloro-5-fluoro-4-piperidin-1-yl-pyrimidine 
• 137890-00-7 2-Chloro-10-(toluene-4-sulfonyl)-pyrimido[4,5-b]indolizine 
• 37554-70-4 2-chloro-5-fluoro-4-methoxy-pyrimidine 
• 81560-11-4 2-chloro-4-benzyloxy-5-fluoropyrimidine 
• 58090-53-2 2,4-di-tert-butoxy-5-fluoropyrimidine 
• 85326-28-9 2,4-Di-sec-butoxy-5-fluoro-pyrimidine 
• 86984-18-1 2,4-dichloro-5-fluoro-6-phenyl-1,6-dihydropyrimidine 
• 22462-40-4 2-chloro-4-(ethylthio)-5-fluoropyrimidine 
• 51-21-8 5-fluorouracil 
• 155-10-2 2-chloro-5-fluoropyrimidin-4-amine 
• 62802-42-0 2-chloro-5-fluoropyrimidine 
• 280581-64-8 2-chloro-5-fluoro-N-phenylpyrimidin-4-amine 
• 155-12-4 2-chloro-5-fluoro-4-hydroxypyrimidine 

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