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41186-03-2

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41186-03-2 Usage

Chemical Properties

clear colorless to yellow viscous liquid

Uses

1-(3-Methylphenyl)piperazine is used in preparation of (2,5-Dioxopyrrolidin-L-yl)(phenyl)acetamide derivatives useful in treatment of neurological disorders.

Check Digit Verification of cas no

The CAS Registry Mumber 41186-03-2 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 4,1,1,8 and 6 respectively; the second part has 2 digits, 0 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 41186-03:
(7*4)+(6*1)+(5*1)+(4*8)+(3*6)+(2*0)+(1*3)=92
92 % 10 = 2
So 41186-03-2 is a valid CAS Registry Number.
InChI:InChI=1/C11H16N2/c1-10-3-2-4-11(9-10)13-7-5-12-6-8-13/h2-4,9,12H,5-8H2,1H3

41186-03-2 Well-known Company Product Price

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  • Aldrich

  • (779822)  1-(3-Methylphenyl)piperazine  ≥97.5% (HPLC)

  • 41186-03-2

  • 779822-10G

  • 651.69CNY

  • Detail

41186-03-2Synthetic route

1-(m-tolyl)piperazine hydrochloride
13078-13-2

1-(m-tolyl)piperazine hydrochloride

1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

Conditions
ConditionsYield
With sodium hydroxide In water at 20℃; for 0.5h; pH=11 - 12;92%
piperazine
110-85-0

piperazine

1-chloro-3-methylbenzene
108-41-8

1-chloro-3-methylbenzene

1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

Conditions
ConditionsYield
Stage #1: piperazine With [2,2]bipyridinyl; tert-Amyl alcohol; nickel diacetate In tetrahydrofuran at 63℃; for 2h; complex formation;
Stage #2: 1-chloro-3-methylbenzene With styrene In tetrahydrofuran for 6h; Arylation; Heating;
82%
piperazine
110-85-0

piperazine

1-chloro-3-methylbenzene
108-41-8

1-chloro-3-methylbenzene

A

1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

B

1,4-bis(3-methylphenyl)piperazine
3477-33-6

1,4-bis(3-methylphenyl)piperazine

Conditions
ConditionsYield
Stage #1: piperazine With [2,2]bipyridinyl; nickel diacetate; sodium hydride; tert-Amyl alcohol In tetrahydrofuran at 65℃; for 2h;
Stage #2: 1-chloro-3-methylbenzene With styrene In tetrahydrofuran at 65℃; for 6h;
A 82%
B 9%
Stage #1: piperazine With [2,2]bipyridinyl; tert-Amyl alcohol; nickel diacetate In tetrahydrofuran at 63℃; for 2h; complex formation;
Stage #2: 1-chloro-3-methylbenzene With styrene In tetrahydrofuran for 9h; Arylation; Heating;
A 57%
B 15%
Stage #1: piperazine With [2,2]bipyridinyl; nickel diacetate; sodium hydride; tert-Amyl alcohol In tetrahydrofuran at 65℃; for 2h;
Stage #2: 1-chloro-3-methylbenzene With styrene In tetrahydrofuran at 65℃; for 9h;
A 57%
B 15%
2,2'-iminobis[ethanol]
111-42-2

2,2'-iminobis[ethanol]

1-amino-3-methylbenzene
108-44-1

1-amino-3-methylbenzene

1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

Conditions
ConditionsYield
With hydrogenchloride for 0.35h; Irradiation;50.3%
25%
piperazine
110-85-0

piperazine

3-Iodotoluene
625-95-6

3-Iodotoluene

1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

Conditions
ConditionsYield
With potassium dihydrogenphosphate; copper(l) iodide In 1,2-dimethoxyethane; isopropyl alcohol for 18h; Reflux; Inert atmosphere;23%
piperazine
110-85-0

piperazine

meta-bromotoluene
591-17-3

meta-bromotoluene

A

1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

B

1,4-bis(3-methylphenyl)piperazine
3477-33-6

1,4-bis(3-methylphenyl)piperazine

C

toluene
108-88-3

toluene

Conditions
ConditionsYield
With sodium t-butanolate; palladium bis(dibenzylideneacetone)palladium(0); tri-tert-butyl phosphine In o-xylene at 120℃; Yield given. Yields of byproduct given;
m-toluidine hydrochloride
638-03-9

m-toluidine hydrochloride

bis-<2-hydroxy-ethyl>-amine hydrochloride

bis-<2-hydroxy-ethyl>-amine hydrochloride

1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

bis-(2-chloroethyl)amine hydrochloride
821-48-7

bis-(2-chloroethyl)amine hydrochloride

1-amino-3-methylbenzene
108-44-1

1-amino-3-methylbenzene

1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

Conditions
ConditionsYield
With potassium carbonate In butan-1-ol for 28h; Reflux;
1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

2-(((3,5-dimethylisoxazol-4-yl)methyl)thio)acetic acid

2-(((3,5-dimethylisoxazol-4-yl)methyl)thio)acetic acid

2-(((3,5-dimethylisoxazol-4-yl)methyl)thio)-1-(4-(m-tolyl)piperazin-1-yl)ethanone

2-(((3,5-dimethylisoxazol-4-yl)methyl)thio)-1-(4-(m-tolyl)piperazin-1-yl)ethanone

Conditions
ConditionsYield
With 2,4,6-tripropyl-1,3,5,2,4,6-trioxatriphosphinane-2,4,6-trioxide; triethylamine In dichloromethane; ethyl acetate at 0 - 20℃; for 48h;96%
1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

methyl (2E)-3-(3-fluoro-2-((((2-methoxy-5-(trifluoromethyl)phenyl)imino)methylene)amino)phenyl)acrylate

methyl (2E)-3-(3-fluoro-2-((((2-methoxy-5-(trifluoromethyl)phenyl)imino)methylene)amino)phenyl)acrylate

{8-fluoro-2-[4-(3-methylphenyl)-1-piperazinyl]-3-[2-methoxy-5-(trifluoromethyl)-phenyl]-3,4-dihydro-4-quinazolinyl}-acetic acid methyl ester

{8-fluoro-2-[4-(3-methylphenyl)-1-piperazinyl]-3-[2-methoxy-5-(trifluoromethyl)-phenyl]-3,4-dihydro-4-quinazolinyl}-acetic acid methyl ester

Conditions
ConditionsYield
In dichloromethane at 20℃; for 21h; Silica gel;95%
1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

1-(2-(oxiran-2-ylmethoxy)phenyl)-3-phenylpropan-1-one
22525-95-7

1-(2-(oxiran-2-ylmethoxy)phenyl)-3-phenylpropan-1-one

C29H34N2O3*ClH

C29H34N2O3*ClH

Conditions
ConditionsYield
Stage #1: 1-(3-Methylphenyl)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
95%
1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

2,6-Dimethyl-4-(4-oxiranylmethoxy-phenyl)-1,4-dihydro-pyridine-3,5-dicarboxylic acid diethyl ester
58259-45-3

2,6-Dimethyl-4-(4-oxiranylmethoxy-phenyl)-1,4-dihydro-pyridine-3,5-dicarboxylic acid diethyl ester

4-{4-[2-Hydroxy-3-(4-m-tolyl-piperazin-1-yl)-propoxy]-phenyl}-2,6-dimethyl-1,4-dihydro-pyridine-3,5-dicarboxylic acid diethyl ester

4-{4-[2-Hydroxy-3-(4-m-tolyl-piperazin-1-yl)-propoxy]-phenyl}-2,6-dimethyl-1,4-dihydro-pyridine-3,5-dicarboxylic acid diethyl ester

Conditions
ConditionsYield
In benzene for 6h; Heating;94%
1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

C18H17FO3
1341230-20-3

C18H17FO3

C29H33FN2O3*ClH

C29H33FN2O3*ClH

Conditions
ConditionsYield
Stage #1: 1-(3-Methylphenyl)piperazine; C18H17FO3 In ethanol at 160℃; for 0.25h; Microwave irradiation;
Stage #2: With hydrogenchloride In methanol
94%
1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

N-(dihydro-3,3-diphenyl-2(3H)-furanylidene)-N-methylmethanaminium bromide
37743-18-3

N-(dihydro-3,3-diphenyl-2(3H)-furanylidene)-N-methylmethanaminium bromide

N,N-dimethyl-2,2-diphenyl-4-(4-m-tolyl-piperazin-1-yl)-butyramide

N,N-dimethyl-2,2-diphenyl-4-(4-m-tolyl-piperazin-1-yl)-butyramide

Conditions
ConditionsYield
With sodium carbonate In N,N-dimethyl-formamide at 100℃; for 4h;93%
1-(4-acetamido-2-methoxyphenoxy)-3-(p-toluenesulfonyloxy)-n-propane
80194-40-7

1-(4-acetamido-2-methoxyphenoxy)-3-(p-toluenesulfonyloxy)-n-propane

1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

1-[3-(4-acetamido-2-methoxyphenoxy)-n-propyl]-4-(3-methylphenyl)-piperazine

1-[3-(4-acetamido-2-methoxyphenoxy)-n-propyl]-4-(3-methylphenyl)-piperazine

Conditions
ConditionsYield
With triethylamine In ethanol92.1%
1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

C18H17FO3
1341230-21-4

C18H17FO3

C29H33FN2O3*ClH

C29H33FN2O3*ClH

Conditions
ConditionsYield
Stage #1: 1-(3-Methylphenyl)piperazine; C18H17FO3 In ethanol at 160℃; for 0.25h; Microwave irradiation;
Stage #2: With hydrogenchloride In methanol
92%
1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

C18H16F2O3
1341230-22-5

C18H16F2O3

C29H32F2N2O3*ClH

C29H32F2N2O3*ClH

Conditions
ConditionsYield
Stage #1: 1-(3-Methylphenyl)piperazine; C18H16F2O3 In ethanol at 160℃; for 0.25h; Microwave irradiation;
Stage #2: With hydrogenchloride In methanol
92%
1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

1-(3-chloro-2-oxopropyl)-2,5-pyrrolidinedione
85834-38-4

1-(3-chloro-2-oxopropyl)-2,5-pyrrolidinedione

1-[2-Oxo-3-(4-m-tolyl-piperazin-1-yl)-propyl]-pyrrolidine-2,5-dione

1-[2-Oxo-3-(4-m-tolyl-piperazin-1-yl)-propyl]-pyrrolidine-2,5-dione

Conditions
ConditionsYield
With triethylamine In acetonitrile for 1h;91.37%
formaldehyd
50-00-0

formaldehyd

1-(2-hydroxyphenyl)-3-phenyl-1,3-propanedione
1469-94-9

1-(2-hydroxyphenyl)-3-phenyl-1,3-propanedione

1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

12,14-Dibenzoyl-14-hydroxymethyl-2,4-dioxa-tricyclo[14.4.0.05,10]icosa-1(20),5(10),6,8,16,18-hexaene-11,15-dione; compound with 1-m-tolyl-piperazine
117609-10-6

12,14-Dibenzoyl-14-hydroxymethyl-2,4-dioxa-tricyclo[14.4.0.05,10]icosa-1(20),5(10),6,8,16,18-hexaene-11,15-dione; compound with 1-m-tolyl-piperazine

Conditions
ConditionsYield
In ethanol Ambient temperature;91%
1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

ibuprofen
15687-27-1

ibuprofen

2-(4-isobutylphenyl)-1-(4-(m-tolyl)piperazin-1-yl)propan-1-one

2-(4-isobutylphenyl)-1-(4-(m-tolyl)piperazin-1-yl)propan-1-one

Conditions
ConditionsYield
Stage #1: ibuprofen With benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In acetonitrile at 20℃; for 0.5h;
Stage #2: 1-(3-Methylphenyl)piperazine In acetonitrile at 20℃; for 12h;
91%
1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

3-(4-methoxyphenyl)pentenedioic anhydride
29199-18-6

3-(4-methoxyphenyl)pentenedioic anhydride

(E)-3-(4-Methoxy-phenyl)-1-(4-m-tolyl-piperazin-1-yl)-but-2-en-1-one

(E)-3-(4-Methoxy-phenyl)-1-(4-m-tolyl-piperazin-1-yl)-but-2-en-1-one

Conditions
ConditionsYield
for 12h; Heating;90%
ethyl-N-(6-fluoro-2-methoxyquinoxaline-3-yl)carbonate

ethyl-N-(6-fluoro-2-methoxyquinoxaline-3-yl)carbonate

1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

1-[(6-fluoro-2-methoxyquinoxalin-3-yl)aminocarbonyl]-4-(3-methylphenyl)piperazine

1-[(6-fluoro-2-methoxyquinoxalin-3-yl)aminocarbonyl]-4-(3-methylphenyl)piperazine

Conditions
ConditionsYield
With 1,8-diazabicyclo[5.4.0]undec-7-ene In tetrahydrofuran at 60℃; for 27h;90%
1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

1-(p-bromophenyl)prop-2-en-1-ol
58824-56-9

1-(p-bromophenyl)prop-2-en-1-ol

(S)-1-(4-bromophenyl)-3-(4-(m-tolyl)piperazin-1-yl)propan-1-ol

(S)-1-(4-bromophenyl)-3-(4-(m-tolyl)piperazin-1-yl)propan-1-ol

Conditions
ConditionsYield
With C55H55ClN2O2P2Ru In toluene at 30℃; for 72h; Inert atmosphere;89%
With potassium phosphate; chloro{(R)-(+)-2,2'-bis[di(3,5-xylyl)phosphino]-1,1'-binaphthyl}[(2R)-(-)-1-(4-methoxyphenyl)-1'-(4-methoxyphenyl-kC)-3-methyl-1,2-butanediamine]ruthenium(II) In toluene at 30℃; for 72h; Inert atmosphere; Sealed tube; enantioselective reaction;89%
1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

4-chloro-3-nitro-benzoyl chloride
38818-50-7

4-chloro-3-nitro-benzoyl chloride

(4-chloro-3-nitrophenyl)(4-(m-tolyl)piperazin-1-yl)-methanone

(4-chloro-3-nitrophenyl)(4-(m-tolyl)piperazin-1-yl)-methanone

Conditions
ConditionsYield
With triethylamine In tetrahydrofuran at 20℃; for 16h;89%
1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

γ-chloropropyl-4-acetamidophenyl sulphide
78234-11-4

γ-chloropropyl-4-acetamidophenyl sulphide

1-<4-(3-methylphenyl)piperazin-1-yl>-3-(4-acetamidophenylthio)propane
139266-11-8

1-<4-(3-methylphenyl)piperazin-1-yl>-3-(4-acetamidophenylthio)propane

Conditions
ConditionsYield
With sodium carbonate; sodium iodide In N,N-dimethyl-formamide88%
With sodium carbonate; sodium iodide In N,N-dimethyl-formamide Condensation;
1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

(3aR,4R,5R,7S,8S,9R,9aS,12R)-8-hydroxy-4,7,9,12-tetramethyl-3-oxo-7-vinyldecahydro-4,9a-propanocyclopenta[8]annulen-5-yl 2-((2-(2-chloroacetamido)phenyl)thio)acetate

(3aR,4R,5R,7S,8S,9R,9aS,12R)-8-hydroxy-4,7,9,12-tetramethyl-3-oxo-7-vinyldecahydro-4,9a-propanocyclopenta[8]annulen-5-yl 2-((2-(2-chloroacetamido)phenyl)thio)acetate

(3aR,4R,5R,7S,8S,9R,9aS,12R)-8-hydroxy-4,7,9,12-tetramethyl-3-oxo-7-vinyldecahydro-4,9a-propanocyclopenta[8]annulen-5-yl 2-((2-(2-(4-(m-tolyl)piperazin-1-yl)acetamido)phenyl)thio)acetate

(3aR,4R,5R,7S,8S,9R,9aS,12R)-8-hydroxy-4,7,9,12-tetramethyl-3-oxo-7-vinyldecahydro-4,9a-propanocyclopenta[8]annulen-5-yl 2-((2-(2-(4-(m-tolyl)piperazin-1-yl)acetamido)phenyl)thio)acetate

Conditions
ConditionsYield
With triethylamine In ethyl acetate at 70℃; for 1h;87.39%
With potassium carbonate In acetonitrile at 70℃; for 3h;40.5%
1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

1-[(3-chloropropyl)thio]-4-fluorobenzene
5322-56-5

1-[(3-chloropropyl)thio]-4-fluorobenzene

1-[3-(4-fluoro-phenylsulfanyl)-propyl]-4-m-tolyl-piperazine

1-[3-(4-fluoro-phenylsulfanyl)-propyl]-4-m-tolyl-piperazine

Conditions
ConditionsYield
With sodium carbonate; sodium iodide In N,N-dimethyl-formamide at 75℃; for 48h;87.2%
1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

2-(2,5-dioxopyrrolidin-1-yl)propanoic acid
73323-90-7

2-(2,5-dioxopyrrolidin-1-yl)propanoic acid

1-{1-[4-(3-methylphenyl)piperazin-1-yl]-1-oxopropan-2-yl}pyrrolidine-2,5-dione

1-{1-[4-(3-methylphenyl)piperazin-1-yl]-1-oxopropan-2-yl}pyrrolidine-2,5-dione

Conditions
ConditionsYield
With 1,1'-carbonyldiimidazole In tetrahydrofuran at 20℃;86%
1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

ethyl acrylate
140-88-5

ethyl acrylate

3-(4-m-tolyl-piperazino)-propionic acid ethyl ester
80428-88-2

3-(4-m-tolyl-piperazino)-propionic acid ethyl ester

Conditions
ConditionsYield
With acetic acid85.5%
With benzene
1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

α-hydroxymethylenedeoxyvasicin-4-one
62062-74-2

α-hydroxymethylenedeoxyvasicin-4-one

α-4-m-tolylpiperazinemethylenedeoxyvasicinone

α-4-m-tolylpiperazinemethylenedeoxyvasicinone

Conditions
ConditionsYield
With sodium hydrogencarbonate In chloroform for 3h; Heating; various conditions;84%
formaldehyd
50-00-0

formaldehyd

1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

3-phenylpyrrolidine-2,5-dione
3464-18-4

3-phenylpyrrolidine-2,5-dione

C22H25N3O2
1262047-58-4

C22H25N3O2

Conditions
ConditionsYield
In ethanol; water at 20℃; Mannich type reaction;84%
4-(chloroacetyl)biphenyl
635-84-7

4-(chloroacetyl)biphenyl

1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

1-(biphenyl-4-yl)-2-(4-m-tolylpiperazin-1-yl)ethanone
1574569-80-4

1-(biphenyl-4-yl)-2-(4-m-tolylpiperazin-1-yl)ethanone

Conditions
ConditionsYield
With potassium carbonate In N,N-dimethyl-formamide at 60℃;84%
1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

1-(2,3-epoxypropyl)-2,5-pyrrolidinedione
20958-21-8

1-(2,3-epoxypropyl)-2,5-pyrrolidinedione

1-[2-Hydroxy-3-(4-m-tolyl-piperazin-1-yl)-propyl]-pyrrolidine-2,5-dione

1-[2-Hydroxy-3-(4-m-tolyl-piperazin-1-yl)-propyl]-pyrrolidine-2,5-dione

Conditions
ConditionsYield
In benzene for 4h; Heating;83.76%
11-chloro-dibenz<1,4>oxazepine
62469-61-8

11-chloro-dibenz<1,4>oxazepine

1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

C24H23N3O

C24H23N3O

Conditions
ConditionsYield
In xylene Heating;83%
formaldehyd
50-00-0

formaldehyd

1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

3-benzhydrylpyrrolidine-2,5-dione
1348753-97-8

3-benzhydrylpyrrolidine-2,5-dione

N-[{4-(3-methylphenyl)piperazin-1-yl}methyl]-3-benzhydrylpyrrolidine-2,5-dione

N-[{4-(3-methylphenyl)piperazin-1-yl}methyl]-3-benzhydrylpyrrolidine-2,5-dione

Conditions
ConditionsYield
In ethanol at 20℃; for 12h;83%
1,4-dibromo-butane
110-52-1

1,4-dibromo-butane

1-(3-Methylphenyl)piperazine
41186-03-2

1-(3-Methylphenyl)piperazine

Br(1-)*C15H23N2(1+)

Br(1-)*C15H23N2(1+)

Conditions
ConditionsYield
With sodium hydrogencarbonate In ethanol for 24h; Reflux; Inert atmosphere;83%

41186-03-2Relevant articles and documents

Synthesis, in vitro cytotoxicity and biological evaluation of twenty novel 1,3-benzenedisulfonyl piperazines as antiplatelet agents

Liu, Xiu-jie,Wang, Yan,Wang, Xiao,Zhang, Zhi-hao

, (2021/09/10)

In order to discover antiplatelet drug with novel structure and expand our research scope, total twenty 1,3-benzenedisulfonyl piperazines, were designed and synthesized. These target compounds were divided into two series, namely 4-methoxy-1,3-benzenedisulfonyl piperazines of series 1 and 4-ethoxy-1,3-benzenedisulfonyl piperazines of series 2. With adenosine diphosphate (ADP), arachidonic acid (AA) and collagen as inducers, respectively, the Born turbidimetric method was used to screen the antiplatelet activity in vitro of all target compounds at a concentration of 1.3 μM, with aspirin and picotamide as positive control drugs. And of which, the activities of five compounds for collagen were higher than both picotamide and aspirin. In ADP or AA channel, compounds with an inhibition rate greater than 33% were selected, and their corresponding IC50 values were obtained. According to the IC50, the in vitro activity of one compound for ADP was higher than picotamide, and for AA, two compounds were higher than two positive control drugs and other two compounds only higher than or equal to aspirin. The preliminary analysis of the structure-activity relationship of the target compounds involved in this study was completed. Further, eight compounds exhibiting higher activity in one or two test channels, were subjected to cytotoxicity test on mouse fibroblasts (L929) by CCK-8 method. The in vitro cytotoxicity of most test compounds showed less than or same to control drug picotamide at 10 μM, but at the higher concentration of 100 μM, merely two compounds exhibited higher cell survival rate than that of picotamide. In addition, compound N1,N3-di(4-ethoxy-1,3-phenylenedisulfonyl)bis(1-(m-tolyl)piperazine), which is delivery activity in the three test channels, and another compound N1,N3–di(4-methoxy-1,3-phenylenedisulfonyl)bis(1-(m-tolyl)piperazine), which has the lowest cytotoxic in vitro compound among series 1 and series 2, respectively, are found and selected for simulation analysis as two most likely to dock with the receptor P2Y12. Each of synthesized compounds in silico molecular property and ADME (absorption, distribution, metabolism and excretion) are predicted by using Molinspiration property engine v2018.10 and PreADMET online servers, respectively. Compared with other series of compounds in the previous stage, the two series compounds obtained after the introduction of piperazinyl have a similar in vitro activity.

ANTI-PAIN COMPOUND AND PREPARATION METHOD THEREFOR

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Paragraph 0071-0073, (2020/11/23)

Disclosed are a compound represented by the general Formula (I), or a stereisomer, tautomer, derivative, prodrug or pharmaceutically acceptable salt thereof, and a method for preparing the compound and use of the compound in manufacture of a medicament for treating a neuropathic pain and/or neuropathic pain syndrome or a medicament for combating an inflammation: wherein R1 is selected from hydrogen, halogen, alkyl, cyano and haloalkyl, R2 and R3 are independently selected from hydrogen, halogen, alkyl, haloalkyl and nitro, and R1, R2 and R3 are not hydrogen at the same time; furthermore, when either R2 or R3 is nitro or halogen, the other two of R1, R2 and R3 are not hydrogen at the same time. The compound has good effects in treating a neuropathic pain and/or neuropathic pain syndrome and good effects in combating an inflammation, and has not side effects such as addiction.

Design, synthesis, and biological evaluation of structurally constrained hybrid analogues containing ropinirole moiety as a novel class of potent and selective dopamine D3 receptor ligands

Zhou, Benhua,Hong, Kwon Ho,Ji, Min,Cai, Jin

, p. 1597 - 1609 (2018/07/31)

Two series of hybrid analogues were designed, synthesized, and evaluated as a novel class of selective ligands for the dopamine D3 receptor. Binding affinities of target compounds were determined (using the method of radioligand binding assay). Compared to comparator agent BP897, compounds 2a and 2c were found to demonstrate a considerable binding affinity and selectivity for D3 receptor, and especially compound 2h was similarly potent and more selective D3R ligand than BP897, a positive reference. Thus, they may provide valuable information for the discovery and development of highly potent dopamine D3 receptor ligands with outstanding selectivity.

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