2252-63-3

Basic information

• Product Name: 1-(4-Fluorophenyl)piperazine
• Synonyms: 4-(1-Piperazino)fluorobenzene;1-(4-Fluorophenyl)piperazine 97%;1-(4-Fluorophenyl)piperazine97%;FLUOROPHENYL PIPERAZINE;TRIFLUOROETHOXY FLUOROPHENYL PIPERAZINE;1-(4-Fluorophenyl)piperazine ,98%;4-(4-Fluorophenyl)piperazine;1-(4-Fluorophenyl)piperazine, 98% 10GR
• CAS NO: 2252-63-3
• Molecular Formula: C₁₀H₁₃FN₂
• Molecular Weight: 180.22
• EINECS: 218-846-6
• Product Categories: Nitrogen cyclic compounds;Piperidines, Piperidones, Piperazines;Piperaizine;API intermediates;Building Blocks;Heterocyclic Building Blocks;Piperazines;Aromatics;Heterocycles;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;Bioactive Small Molecules;Building Blocks;C10;Cell Biology;Chemical Synthesis;F;Fluorinated Building Blocks;Heterocyclic Building Blocks;Heterocyclic Fluorinated Building Blocks;Other Fluorinated Heterocycles
• Mol File: 2252-63-3.mol
• Article Data: 24

Chemical Properties

• Melting Point: 30-33 °C(lit.)
• Boiling Point: 118-123 °C0.1 mm Hg(lit.)
• Flash Point: >230 °F
• Appearance: Clear yellow/Liquid After Melting
• Density: 1.0
• Vapor Pressure: 1.78E-05mmHg at 25°C
• Refractive Index: 1.5585-1.5605
• Storage Temp.: Refrigerator
• PKA: 8.93±0.10(Predicted)
• Water Solubility: Insoluble in water.
• Sensitive: Air Sensitive
• BRN: 610723
• CAS DataBase Reference: 1-(4-Fluorophenyl)piperazine(CAS DataBase Reference)
• NIST Chemistry Reference: 1-(4-Fluorophenyl)piperazine(2252-63-3)
• EPA Substance Registry System: 1-(4-Fluorophenyl)piperazine(2252-63-3)

Safety Data

• Hazard Codes: Xn,T,C
• Statements: 22-36/37/38-20/21/22
• Safety Statements: 26-36
• RIDADR: 2811
• WGK Germany: 2
• HazardClass: 8
• PackingGroup: III
• Hazardous Substances Data: 2252-63-3(Hazardous Substances Data)

Usage

Chemical Properties

clear yellowish liquid after melting

Uses

Different sources of media describe the Uses of 2252-63-3 differently. You can refer to the following data:
1. 1-(4-Fluorophenyl)piperazine is a major metabolite of Niaparazine, a sedative, hypnotic drug. Metabolites of Niaprazine occurred by N-dealkylation, N-dearylation, aromatic hydroxylation and N-oxidatio n.
2. 1-(4-Fluorophenyl)piperazine was used in the synthesis of N,N-disubstituted piperazine. It is a major metabolite of niaparazine, a sedative, a hypnotic drug.

InChI:InChI=1/C10H13FN2/c11-9-1-3-10(4-2-9)13-7-5-12-6-8-13/h1-4,12H,5-8H2/p+1

Synthetic route

piperazine (110-85-0) + NaOBut + tri-tert-butyl phosphine (13716-12-6) + 1-Bromo-4-fluorobenzene (460-00-4) → 1-(4-Fluorophenyl)piperazine (2252-63-3)

Conditions	Yield
palladium diacetate In o-xylene; water	95%

piperazine (110-85-0) + 1-Chloro-4-fluorobenzene (352-33-0) → 1-(4-Fluorophenyl)piperazine (2252-63-3)

Conditions	Yield
With tris-(dibenzylideneacetone)dipalladium(0); 2-dicyclohexylphosphino-2′,6′-di-i-propoxy-1,1′-biphenyl; sodium t-butanolate In 1,4-dioxane at 100℃; for 0.166667h; Temperature;	88%
With tris-(dibenzylideneacetone)dipalladium(0); sodium t-butanolate; ruphos In 1,4-dioxane at 100℃; for 1h; Buchwald-Hartwig Coupling;	81.1%

bis-(2-chloroethyl)amine hydrochloride (821-48-7) + 4-fluoroaniline (371-40-4) → 1-(4-Fluorophenyl)piperazine (2252-63-3)

Conditions	Yield
In various solvent(s) at 150℃;	87%
With toluene-4-sulfonic acid at 145℃;
With potassium iodide at 150℃; Inert atmosphere;

tert-butyl 4-(4-fluorophenyl)piperazine-1-carboxylate (141940-39-8) → 1-(4-Fluorophenyl)piperazine (2252-63-3)

Conditions	Yield
With trifluoroacetic acid In dichloromethane at 20℃; for 2h;	83%

4-(4-fluorophenyl)-1-toluene-p-sulfonylpiperazine (4004-97-1) → 1-(4-Fluorophenyl)piperazine (2252-63-3)

Conditions	Yield
With hydrogen bromide; phenol for 0.5h; Heating;	66%

2-bromo-N(2-bromoethyl)-N-carbethoxy-ethanamine (77697-11-1) + 4-fluoroaniline (371-40-4) → 1-(4-Fluorophenyl)piperazine (2252-63-3)

Conditions	Yield
With methanol; basic alumina (Waters Sep-Pak cartridge 51820) at 150℃; for 0.666667h;	75 % Chromat.
With methanol; aluminum oxide at 150℃; for 0.666667h; Product distribution; reaction of aniline derivatives with bis(2-bromoethyl)-N-(ethoxycarbonyl)amine on solid support;	75 % Chromat.

piperazine (110-85-0) + 1-Bromo-4-fluorobenzene (460-00-4) → fluorobenzene (462-06-6) + 1-(4-Fluorophenyl)piperazine (2252-63-3) + 1,4-bis-(4-fluoro-phenyl)-piperazine (21598-27-6)

Conditions	Yield
With sodium t-butanolate; palladium bis(dibenzylideneacetone)palladium(0); tri-tert-butyl phosphine In o-xylene at 120℃; Yield given. Yields of byproduct given;

1-Bromo-4-fluorobenzene (460-00-4) → fluorobenzene (462-06-6) + 1-(4-Fluorophenyl)piperazine (2252-63-3) + 1,4-bis-(4-fluoro-phenyl)-piperazine (21598-27-6)

Conditions	Yield
With piperazine; sodium t-butanolate; palladium diacetate; tri-tert-butyl phosphine In o-xylene at 120℃; Yield given. Yields of byproduct given;

piperazine (110-85-0) + 1-Bromo-4-fluorobenzene (460-00-4) → 1-(4-Fluorophenyl)piperazine (2252-63-3)

Conditions	Yield
With dichlorobis(tri-O-tolylphosphine)palladium; sodium t-butanolate In toluene Heating;
Buchwald-Hartwig amination;
With palladium diacetate; Tri(p-tolyl)phosphine; sodium t-butanolate In toluene at 110℃;
Stage #1: piperazine With palladium diacetate; 2,2'-bis-(diphenylphosphino)-1,1'-binaphthyl; sodium t-butanolate In toluene at 20℃; for 0.25h; Buchwald-Hartwig Coupling; Inert atmosphere; Stage #2: 1-Bromo-4-fluorobenzene In toluene for 20h; Buchwald-Hartwig Coupling; Inert atmosphere; Reflux;

VersabeadsTM VO400-bound bis(chloroethyl)amine + 4-fluoroaniline (371-40-4) → 1-(4-Fluorophenyl)piperazine (2252-63-3)

Conditions	Yield
Stage #1: VersabeadsTM VO400-bound bis(chloroethyl)amine; 4-fluoroaniline With pyridine; potassium iodide at 100℃; for 66h; Stage #2: With potassium tert-butylate In 1,2-dimethoxyethane for 3h; Heating;

4-fluoroaniline (371-40-4) + alkali thiocyanate → 1-(4-Fluorophenyl)piperazine (2252-63-3)

Conditions	Yield
Multi-step reaction with 2 steps 1: 58 percent / NaHCO3, HMPA / 1 h / 130 °C 2: 66 percent / 48percent aq. HBr, phenol / 0.5 h / Heating View Scheme

tris-(o-tolyl)phosphine (6163-58-2) + 1-Bromo-4-fluorobenzene (460-00-4) → 1-(4-Fluorophenyl)piperazine (2252-63-3)

Conditions	Yield
tris-(dibenzylideneacetone)dipalladium(0)

cycl-isopropylidene malonate (2033-24-1) + 2,3,4,6,7,8,9,10-octahydropyrimido<1,2-a>azepino (5768-55-8) → 3-(3-(4-(4-fluorophenyl)piperazin-1-yl)propyl)-6,7,8,9-tetrahydro-5H-imidazo[1,2-a]azepine + 1-(4-Fluorophenyl)piperazine (2252-63-3)

1-t-Butoxycarbonylpiperazine (57260-71-6) + 1-halide-4-fluorobenzene → 1-(4-Fluorophenyl)piperazine (2252-63-3)

Conditions	Yield
Stage #1: 1-t-Butoxycarbonylpiperazine; 1-halide-4-fluorobenzene Buchwald-Hartwig cross coupling; Stage #2: With hydrogenchloride In 1,4-dioxane

fluorobenzene (462-06-6) + Selectfluor (140681-55-6) → 1-(4-Fluorophenyl)piperazine (2252-63-3)

Conditions	Yield
Multi-step reaction with 2 steps 1: C20H28N4O2Pd(2+)*2BF4(1-); tris(2,2-bipyridine)ruthenium(II) hexafluorophosphate / acetonitrile / 24 h 2: sodium thiosulfate; water / acetonitrile / 2 h / Sealed tube View Scheme

C13H18ClFN2(2+)*2BF4(1-) → 1-(4-Fluorophenyl)piperazine (2252-63-3)

Conditions	Yield
With water; sodium thiosulfate In acetonitrile for 2h; Sealed tube;

1-Bromo-4-fluorobenzene (460-00-4) → 1-(4-Fluorophenyl)piperazine (2252-63-3)

Conditions	Yield
Multi-step reaction with 2 steps 1: 2,2'-bis-(diphenylphosphino)-1,1'-binaphthyl; palladium diacetate; sodium t-butanolate / toluene / 8.83 h / 100 °C / Inert atmosphere 2: trifluoroacetic acid / dichloromethane / 2 h / 20 °C View Scheme

(E)-11-(2-chloroethylidene)-6,11-dihydrodibenzoxepin-2-carboxylic acid methyl ester (127167-47-9) + 1-(4-Fluorophenyl)piperazine (2252-63-3) → 11-[2-[4-(4-Fluoro-phenyl)-piperazin-1-yl]-eth-(E)-ylidene]-6,11-dihydro-dibenzo[b,e]oxepine-2-carboxylic acid methyl ester

Conditions	Yield
In ethanol	100%

1-(4-Fluorophenyl)piperazine (2252-63-3) + N-(4-bromobutyl)-dibenzobicyclo<2.2.2>octane-2,3-dicarboximide → C32H32FN3O2

Conditions	Yield
With potassium carbonate; potassium iodide In acetonitrile for 30h; Heating;	100%

1-(4-Fluorophenyl)piperazine (2252-63-3) + 5-(3-chloropropyl)-1-methyl-1,4,5,6,7,8-hexahydro-pyrrolo[3,2-c]azepine-4,8-dione (191591-69-2) → 5-[3-[4-(4-fluorophenyl)piperazin-1-yl]propyl]-1-methyl-1,4,5,6,7,8-hexahydropyrrolo[3,2-c]azepine-4,8-dione (191591-86-3)

Conditions	Yield
With potassium carbonate; sodium iodide In acetonitrile for 38h; Alkylation; Heating;	100%
With sodium iodide; sodium chloride; potassium carbonate In acetonitrile	99%
With sodium iodide; sodium chloride; potassium carbonate In acetonitrile	99%
With sodium iodide; potassium carbonate In acetonitrile	99%

1-(4-Fluorophenyl)piperazine (2252-63-3) + 7-(4-bromobutyl)-1-methyl-1,4,5,6,7,8-hexahydropyrrolo[2,3-c]azepine-4,8-dione (150159-17-4) → 7-[4-[4-(4-fluorophenyl)piperazin-1-yl]butyl]-1-methyl-1,4,5,6,7,8-hexahydropyrrolo[2,3-c]azepine-4,8-dione

Conditions	Yield
With potassium carbonate; sodium iodide In acetonitrile for 14h; Heating;	100%

6-(2-hydroxyethyl)-2-(methylthio)-4-pyrimidinyl 4-methyl-1-benzenesulfonate (920490-05-7) + 1-(4-Fluorophenyl)piperazine (2252-63-3) → C17H21FN4OS

Conditions	Yield
In tetrahydrofuran at 70℃; for 48h;	100%

N6-Boc-N2-Cbz-lysine (215595-66-7) + 1-(4-Fluorophenyl)piperazine (2252-63-3) → C29H39FN4O5

Conditions	Yield
With triethylamine	100%

(R)-3-(7-methyl-1H-indazol-5-yl)-2-(4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carbonyloxy)propanoic acid (865626-86-4) + 1-(4-Fluorophenyl)piperazine (2252-63-3) → (R)-1-(4-(4-Fluorophenyl)piperazin-1-yl)-3-(7-methyl-1H-indazol-5-yl)-1-oxopropan-2-yl 4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxylate

Conditions	Yield
With benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate; N-ethyl-N,N-diisopropylamine In DMF (N,N-dimethyl-formamide); dichloromethane at 0℃; for 4h;	100%
With benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate; N-ethyl-N,N-diisopropylamine In dichloromethane; N,N-dimethyl-formamide

2-(3-chloropropyl)-6-methyl-3,4,5,6-tetrahydro-2H-pyrrolo[2,3-f][1,2]thiazepin-5-one 1,1-dioxide (232619-87-3) + 1-(4-Fluorophenyl)piperazine (2252-63-3) → 2-[3-[4-(4-fluorophenyl)piperazin-1-yl]propyl]-6-methyl-3,4,5,6-tetrahydro-2H-pyrrolo[2,3-f][1,2]thiazepin-5-one 1,1-dioxide

Conditions	Yield
With sodium iodide; potassium carbonate In acetonitrile	100%

formaldehyd (50-00-0) + 1-(4-Fluorophenyl)piperazine (2252-63-3) → 1-(4-fluorophenyl)-4-methylpiperazine

Conditions	Yield
Heating;	99%

2-(3-bromopropyl)-4,4-dimethoxy-3,4-dihydro-2H-1,2-benzothiazine 1,1-dioxide + 1-(4-Fluorophenyl)piperazine (2252-63-3) → 2-[3-[4-(4-fluorophenyl)piperazin-1-yl]propyl]-4,4-dimethoxy-3,4-dihydro-2H-1,2-benzothiazine 1,1-dioxide

Conditions	Yield
With potassium carbonate In 1,4-dioxane	99%

7-(dimethylamino)methyl-3-methyl-2-pyrrolidin-1-yl-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one (1179358-18-9) + 1-(4-Fluorophenyl)piperazine (2252-63-3) → 7-{[4-(4-fluorophenyl)piperazin-1-yl]methyl}-3-methyl-2-pyrrolidin-1-yl-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one (1179358-24-7)

Conditions	Yield
In toluene at 110℃; for 3h;	99%

(1R,4R)-7,7-dimethyl-1-((R)-oxiran-2-yl)bicyclo[2.2.1]heptan-2-one + 1-(4-Fluorophenyl)piperazine (2252-63-3) → (1R,4R)-1-((R)-2-(4-(4-fluorophenyl)piperazin-1-yl)-1-hydroxyethyl)-7,7-dimethylbicyclo[2.2.1]heptan-2-one (1615687-82-5)

Conditions	Yield
With lithium perchlorate In acetonitrile at 20 - 50℃;	99%

C12H22N2O2 + 1-(4-Fluorophenyl)piperazine (2252-63-3) → C22H35FN4O

Conditions	Yield
With sodium cyanoborohydride; zinc(II) chloride In methanol at 75℃; for 27h;	98.99%

C10H18N2O2 + 1-(4-Fluorophenyl)piperazine (2252-63-3) → C20H31FN4O

Conditions	Yield
With sodium cyanoborohydride; zinc(II) chloride In methanol at 75℃; for 96h;	98.01%

3-(2-bromoethyl)oxazolo<4,5-b>pyridin-2(3H)-one (134336-95-1) + 1-(4-Fluorophenyl)piperazine (2252-63-3) → 3-<2-<4-(4-fluorophenyl)-1-piperazinyl>ethyl>oxazolo<4,5-b>pyridin-2(3H)-one

Conditions	Yield
With N-ethyl-N,N-diisopropylamine In acetonitrile at 60℃; for 12h;	98%

1-(4-Fluorophenyl)piperazine (2252-63-3) + α-hydroxymethylenedeoxyvasicin-4-one (62062-74-2) → 3-[4-(4-fluoro-phenyl)-piperazin-1-ylmethylene]-2,3-dihydro-1H-pyrrolo[2,1-b]quinazolin-9-one

Conditions	Yield
In chloroform Heating; various conditions;	98%

1-(4-Fluorophenyl)piperazine (2252-63-3) + 7,8-difluoro-1-methyl-4-oxo-1,4,5,10-tetrahydro-benzo[b][1,8]naphthyridine-3-carboxylic acid → 7-fluoro-8-[4-(4-fluoro-phenyl)-piperazin-1-yl]-1-methyl-4-oxo-1,4,5,10-tetrahydro-benzo[b][1,8]naphthyridine-3-carboxylic acid

Conditions	Yield
In dimethyl sulfoxide at 90℃; for 4h;	98%

N-(dihydro-3,3-diphenyl-2(3H)-furanylidene)-N-methylmethanaminium bromide (37743-18-3) + 1-(4-Fluorophenyl)piperazine (2252-63-3) → 4-[4-(4-fluoro-phenyl)-piperazin-1-yl]-N,N-dimethyl-2,2-diphenyl-butyramide

Conditions	Yield
With sodium carbonate In N,N-dimethyl-formamide at 100℃; for 4h;	98%

3,4-difluoronitrobenzene (369-34-6) + 1-(4-Fluorophenyl)piperazine (2252-63-3) → 1-(2-fluoro-4-nitrophenyl)-4-(4-fluorophenyl)-piperazine

Conditions	Yield
Stage #1: 1-(4-Fluorophenyl)piperazine With N-ethyl-N,N-diisopropylamine In acetonitrile at 20℃; for 0.5h; Inert atmosphere; Stage #2: 3,4-difluoronitrobenzene In acetonitrile Inert atmosphere; Reflux;	98%
With sodium hydrogencarbonate at 125℃; for 0.5h; Temperature; Microwave irradiation;	90%
With sodium hydrogencarbonate In neat (no solvent) at 125℃; for 0.5h; Microwave irradiation; Sealed tube;	90%
With N-ethyl-N,N-diisopropylamine

2-(3-chloropropyl)-5-methoxy-3,4-dihydro-2H-1,2-benzothiazin-4-one 1,1-dioxide ethylene acetal (186491-71-4) + 1-(4-Fluorophenyl)piperazine (2252-63-3) → 2-[3-[4-(4-fluorophenyl)piperazin-1-yl]propyl]-5-methoxy-3,4-dihydro-2H-1,2-benzothiazin-4-one 1,1-dioxide ethylene acetal (186491-82-7)

Conditions	Yield
With sodium iodide; sodium hydrogencarbonate In acetonitrile	98%

5-chloro-2-(3-chloropropyl)-3,4-dihydro-2H-1,2-benzothiazin-4-one 1,1-dioxide ethylene acetal (186491-72-5) + 1-(4-Fluorophenyl)piperazine (2252-63-3) → 5-chloro-2-[3-[4-(4-fluorophenyl)piperazin-1-yl]propyl]-3,4-dihydro-2H-1,2-benzothiazin-4-one 1,1-dioxide ethylene acetal (186491-85-0)

Conditions	Yield
With sodium iodide; sodium hydrogencarbonate In acetonitrile	98%

(1R,4R)-7,7-dimethyl-1-((S)-oxiran-2-yl)bicyclo[2.2.1]heptan-2-one + 1-(4-Fluorophenyl)piperazine (2252-63-3) → (1R,4R)-1-((S)-2-(4-(4-fluorophenyl)piperazin-1-yl)-1-hydroxyethyl)-7,7-dimethylbicyclo[2.2.1]heptan-2-one (1615687-99-4)

Conditions	Yield
With lithium perchlorate In acetonitrile at 20 - 50℃;	98%

methyl 4-((((4-nitrophenoxy)carbonyl)(pyridine-2-yl)amino)methyl)benzoate + 1-(4-Fluorophenyl)piperazine (2252-63-3) → methyl 4-((4-(4-fluorophenyl)-N-(pyridin-2-yl)piperazine-1-carboxamido)methyl)benzoate

Conditions	Yield
With potassium carbonate In N,N-dimethyl-formamide at 55℃; for 12h;	98%

1-(3-bromopropyl)oxazolo<5,4-b>pyridin-2(1H)-one (142714-73-6) + 1-(4-Fluorophenyl)piperazine (2252-63-3) → 1-<3-<4-(4-fluorophenyl)-1-piperazinyl>propyl>oxazolo<5,4-b>pyridin-2(1H)-one

Conditions	Yield
With N-ethyl-N,N-diisopropylamine In acetonitrile at 85℃; for 12h;	97%

1-(4-Fluorophenyl)piperazine (2252-63-3) + 3-(4-benzyl-3,4-dihydro-2H-1,4-benzoxazin-2-yl)propionic acid (212578-60-4) → 3-(4-Benzyl-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl)-1-[4-(4-fluoro-phenyl)-piperazin-1-yl]-propan-1-one (212578-62-6)

Conditions	Yield
With 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane for 5h; Ambient temperature;	97%

1-(4-Fluorophenyl)piperazine (2252-63-3) + (2R,3S,8R,9S,10S,13S,14S,17S)-10,13-Dimethyl-hexadecahydro-20-oxa-cyclopropa[2,3]cyclopenta[a]phenanthren-17-ol → (2S,3S,8R,9S,10S,13S,14S,17S)-2-[4-(4-Fluoro-phenyl)-piperazin-1-yl]-10,13-dimethyl-hexadecahydro-cyclopenta[a]phenanthrene-3,17-diol

Conditions	Yield
With gadolinium(III) trifluoromethanesulfonate In toluene at 150 - 190℃;	97%

1-(4-Fluorophenyl)piperazine (2252-63-3) + 1-(2-(oxiran-2-ylmethoxy)phenyl)-3-phenylpropan-1-one (22525-95-7) → 1-<2-<3-<4-(4-fluorophenyl)-1-piperazinyl>-2-hydroxypropoxy>phenyl>-3-phenyl-1-propanone hydrochloride

Conditions	Yield
Stage #1: 1-(4-Fluorophenyl)piperazine; 1-(2-(oxiran-2-ylmethoxy)phenyl)-3-phenylpropan-1-one In ethanol at 160℃; for 0.25h; Microwave irradiation; Stage #2: With hydrogenchloride In methanol	97%

1-(4-Fluorophenyl)piperazine (2252-63-3) + Benzyl bromoacetate (5437-45-6) → C19H21FN2O2 (486457-27-6)

Conditions	Yield
With triethylamine; potassium iodide In tetrahydrofuran Reflux;	97%

propargyl alcohol (107-19-7) + 2,2,2-trifluoro-N-(2-iodophenyl)acetamide (143321-89-5) + 1-(4-Fluorophenyl)piperazine (2252-63-3) → 2-((4-(4-fluorophenyl)piperazine-1-yl)methyl)-1H-indole

Conditions	Yield
With bis-triphenylphosphine-palladium(II) chloride; copper(l) iodide; potassium carbonate In N,N-dimethyl-formamide at 80℃; for 2h; Inert atmosphere;	97%

1-(4-Fluorophenyl)piperazine (2252-63-3) + 1-bromomethyl-3-nitrobenzene (3958-57-4) → 1-(4-fluorophenyl)-4-(3-nitrobenzyl)piperazine

Conditions	Yield
With triethylamine In tetrahydrofuran at 20℃;	97%

Upstream product

• 371-40-4 4-fluoroaniline 
• 2033-24-1 cycl-isopropylidene malonate 
• 5768-55-8 2,3,4,6,7,8,9,10-octahydropyrimido<1,2-a>azepino 
• 141940-39-8 tert-butyl 4-(4-fluorophenyl)piperazine-1-carboxylate 
• 460-00-4 1-Bromo-4-fluorobenzene 
• 110-85-0 piperazine 
• 352-33-0 1-Chloro-4-fluorobenzene 
• 462-06-6 fluorobenzene 
• 140681-55-6 Selectfluor 
• 57260-71-6 1-t-Butoxycarbonylpiperazine 
• 13716-12-6 tri-tert-butyl phosphine 
• 6163-58-2 tris-(o-tolyl)phosphine 
• 821-48-7 bis-(2-chloroethyl)amine hydrochloride 
• 77697-11-1 2-bromo-N(2-bromoethyl)-N-carbethoxy-ethanamine 

Downstream Products

• 81513-89-5 3-[4-(4-Fluoro-phenyl)-piperazin-1-ylmethyl]-3H-benzooxazol-2-one 
• 83823-55-6 1-Chroman-3-yl-4-(4-fluoro-phenyl)-piperazine 
• 120301-26-0 2-{4-[4-(4-fluorophenyl)piperazin-1-yl]butyl}-1H-isoindole-1,3(2H)-dione 
• 105173-87-3 3-(4-(4-fluorophenyl)piperazin-1-yl)propan-1-ol 
• 90096-38-1 2-<4-(4-fluorophenyl)piperazin-1-yl>ethanol 
• 188915-08-4 2-{4-[4-(4-Fluoro-phenyl)-piperazin-1-yl]-butyl}-tetrahydro-imidazo[1,5-a]pyridine-1,3-dione 
• 188915-06-2 2-{4-[4-(4-Fluoro-phenyl)-piperazin-1-yl]-butyl}-tetrahydro-pyrrolo[1,2-c]imidazole-1,3-dione 
• 188914-92-3 2-{2-[4-(4-Fluoro-phenyl)-piperazin-1-yl]-ethyl}-tetrahydro-imidazo[1,5-a]pyridine-1,3-dione 

Relevant articles and documents

Synthesis and biological evaluation of novel 3-substituted amino-4-hydroxylcoumarin derivatives as chitin synthase inhibitors and antifungal agents

A series of novel 3-substituted amino-4-hydroxycoumarin derivatives have been designed and synthesized as chitin synthase (CHS) inhibitors. All the synthesized compounds have been screened for their CHS inhibition activity and antimicrobial activity in vitro. The enzymatic assay indicated that most of the compounds have good inhibitory activity against CHS, in which compound 6o with IC50 of 0.10 mmol/L had stronger activity than that of polyoxins B, which acts as control drug with IC50 of 0.18 mmol/L. As far as the antifungal activity is concerned, most of the compounds possessed moderate to excellent activity against some representative pathogenic fungi. Especially, compound 6b was found to be the most potent agent against Cryptococcus neoformans with minimal inhibitory concentration (MIC) of 4 g/mL. Moreover, the results of antibacterial screening showed that these compounds have negligible actions to some tested bacteria. Therefore, these compounds would be promising to develop selective antifungal agents.

7-benzyl-4-(4-phenylpiperazin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine derivatives and Composition for skin whitening and Pharmaceutical composition for use in preventing or treating disorders of Melanin Hyperpigmentation containing the same as an active ingredient

The present invention relates to a 7-benzyl-4(4-phenylpiperazin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine derivative, and to a composition for skin whitening, comprising the same as an active ingredient. Since the derivative exhibits the effect of inhibiting the production of melanin even when used in a small amount, it is useful as a pharmaceutical composition for preventing or treating melanin hyperpigmentation diseases, a cosmetic composition for skin whitening, and a health functional food for skin whitening.

Pd-Catalyzed Synthesis of Piperazine Scaffolds under Aerobic and Solvent-Free Conditions

A facile Pd-catalyzed methodology providing an efficient synthetic route to biologically relevant arylpiperazines under aerobic conditions is reported. Electron donating and sterically hindered aryl chlorides were aminated to afford yields up to 97%, with examples using piperazine as solvent, illustrating an ecofriendly, cost-effective synthesis of these privileged structures.