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122368-54-1

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  • High Quality 99% 2-[(4-Chlorophenyl)(4-Piperidinyloxy)Methyl]-Pyridine 122368-54-1 GMP manufacturer

    Cas No: 122368-54-1

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122368-54-1 Usage

Uses

Different sources of media describe the Uses of 122368-54-1 differently. You can refer to the following data:
1. 2-[(4-Chlorophenyl)(4-piperidinyloxy)methyl]pyridine is an intermediate in the synthesis of Bepotastine besylate, a non-sedating H1-antagonist that has anti-inflammatory activity.
2. 2-[(4-Chlorophenyl)(4-piperidinyloxy)methyl]pyridine is an intermediate in the synthesis of Bepotastine besylate (B317000), a non-sedating H1-antagonist that has anti-inflammatory activity.

Chemical Properties

Brown liquid

Check Digit Verification of cas no

The CAS Registry Mumber 122368-54-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,2,2,3,6 and 8 respectively; the second part has 2 digits, 5 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 122368-54:
(8*1)+(7*2)+(6*2)+(5*3)+(4*6)+(3*8)+(2*5)+(1*4)=111
111 % 10 = 1
So 122368-54-1 is a valid CAS Registry Number.
InChI:InChI=1/C17H19ClN2O/c18-14-6-4-13(5-7-14)17(16-3-1-2-10-20-16)21-15-8-11-19-12-9-15/h1-7,10,15,17,19H,8-9,11-12H2

122368-54-1SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 20, 2017

Revision Date: Aug 20, 2017

1.Identification

1.1 GHS Product identifier

Product name 2-((4-Chlorophenyl)(piperidin-4-yloxy)methyl)pyridine

1.2 Other means of identification

Product number -
Other names 2-[(4-chlorophenyl)-piperidin-4-yloxymethyl]pyridine

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:122368-54-1 SDS

122368-54-1Synthetic route

4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidine fumaric acid salt

4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidine fumaric acid salt

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

Conditions
ConditionsYield
With sodium hydroxide In dichloromethane at 20℃; for 0.166667h;99%
With sodium hydroxide In dichloromethane86.6%
2-((1-benzylpiperidin-4-yloxy)(4-chlorophenyl)methyl)pyridine

2-((1-benzylpiperidin-4-yloxy)(4-chlorophenyl)methyl)pyridine

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

Conditions
ConditionsYield
With 5%-palladium/activated carbon In methanol at 30℃; under 2068.65 Torr; for 4h; Inert atmosphere; Autoclave;94%
3-(4-chlorophenyl)-[1,2,3]triazolo[1,5-a]pyridine
78539-93-2

3-(4-chlorophenyl)-[1,2,3]triazolo[1,5-a]pyridine

t-butyl 4-hydroxy piperidine-1-carboxylate
109384-19-2

t-butyl 4-hydroxy piperidine-1-carboxylate

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

Conditions
ConditionsYield
Stage #1: 3-(4-chlorophenyl)-[1,2,3]triazolo[1,5-a]pyridine; t-butyl 4-hydroxy piperidine-1-carboxylate With potassium carbonate In benzene at 20℃; for 10h; UV-irradiation;
Stage #2: With trifluoroacetic acid at 20℃; for 1h;
71%
(4-chlorophenyl)-2-pyridylmethanol
27652-89-7

(4-chlorophenyl)-2-pyridylmethanol

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1: triethylamine / toluene / 1 h / 0 - 20 °C
2: N-ethyl-N,N-diisopropylamine / 3 h / 80 °C
3: sodium hydroxide / isopropyl alcohol / 12 h / Reflux
4: 5 h / 20 °C
5: sodium hydroxide / dichloromethane / 0.17 h / 20 °C
View Scheme
Multi-step reaction with 2 steps
1: potassium carbonate / N,N-dimethyl-formamide / 20 h / Reflux
2: 5%-palladium/activated carbon / methanol / 4 h / 30 °C / 2068.65 Torr / Inert atmosphere; Autoclave
View Scheme
C13H12ClNO3S

C13H12ClNO3S

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1: N-ethyl-N,N-diisopropylamine / 3 h / 80 °C
2: sodium hydroxide / isopropyl alcohol / 12 h / Reflux
3: 5 h / 20 °C
4: sodium hydroxide / dichloromethane / 0.17 h / 20 °C
View Scheme
4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidine-1-carboxylic acid ethyl ester
207726-35-0

4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidine-1-carboxylic acid ethyl ester

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: sodium hydroxide / isopropyl alcohol / 12 h / Reflux
2: 5 h / 20 °C
3: sodium hydroxide / dichloromethane / 0.17 h / 20 °C
View Scheme
With isopropyl alcohol; sodium hydroxide at 88℃; for 6h;
C18H19ClN2O3

C18H19ClN2O3

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: 5 h / 20 °C
2: sodium hydroxide / dichloromethane / 0.17 h / 20 °C
View Scheme
N-acetyl-4-hydroxypiperidine
4045-22-1

N-acetyl-4-hydroxypiperidine

2-(chloro(4-chlorophenyl)methyl)pyridine
142404-69-1

2-(chloro(4-chlorophenyl)methyl)pyridine

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

Conditions
ConditionsYield
Stage #1: N-acetyl-4-hydroxypiperidine; 2-[chloro(4-chlorophenyl)methyl]pyridine at 130℃; for 5h; Large scale;
Stage #2: With hydrogenchloride In water at 80℃; for 15h; Large scale;
4-HYDROXYPIPERIDINE
5382-16-1

4-HYDROXYPIPERIDINE

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1.1: triethylamine / dichloromethane / 1 h / -70 °C / Large scale
1.2: 20 °C / Large scale
2.1: 5 h / 130 °C / Large scale
2.2: 15 h / 80 °C / Large scale
View Scheme
2-bromo-pyridine
109-04-6

2-bromo-pyridine

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1.1: isopropylmagnesium bromide / tetrahydrofuran / 1 h / 10 - 20 °C / Inert atmosphere
1.2: 4 h / Inert atmosphere
2.1: potassium carbonate / N,N-dimethyl-formamide / 20 h / Reflux
3.1: 5%-palladium/activated carbon / methanol / 4 h / 30 °C / 2068.65 Torr / Inert atmosphere; Autoclave
View Scheme
4-chlorobenzaldehyde
104-88-1

4-chlorobenzaldehyde

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1.1: isopropylmagnesium bromide / tetrahydrofuran / 1 h / 10 - 20 °C / Inert atmosphere
1.2: 4 h / Inert atmosphere
2.1: potassium carbonate / N,N-dimethyl-formamide / 20 h / Reflux
3.1: 5%-palladium/activated carbon / methanol / 4 h / 30 °C / 2068.65 Torr / Inert atmosphere; Autoclave
View Scheme
4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

(R)-(+)-2-((4-chlorophenyl)(piperidin-4-yloxy)methyl)pyridine

(R)-(+)-2-((4-chlorophenyl)(piperidin-4-yloxy)methyl)pyridine

Conditions
ConditionsYield
Stage #1: 4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine With (+)-dibenzoyl-D-tartaric acid monohydrate In acetic acid methyl ester
Stage #2: With D-tartaric acid In ethanol at 20℃;
Stage #3: With sodium hydroxide In water
99.6%
With (R)-Mandelic Acid In methanol at 60℃; for 2h; Reflux;40%
Stage #1: 4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine With (S)-2-acetylamino-3-phenylpropanoic acid In ethyl acetate Heating;
Stage #2: With Cbz-Met-OH In acetonitrile Heating;
38.2%
4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

menthyl 4-chlorobutyrate
668486-64-4

menthyl 4-chlorobutyrate

(R/S)-bepotastine L-menthyl ester
1092777-15-5

(R/S)-bepotastine L-menthyl ester

Conditions
ConditionsYield
Stage #1: menthyl 4-chlorobutyrate With sodium iodide for 5h; Heating / reflux;
Stage #2: 4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine With potassium carbonate for 1h; Product distribution / selectivity; Heating / reflux;
99%
Stage #1: menthyl 4-chlorobutyrate With sodium iodide In 4-methyl-2-pentanone for 5h; Reflux;
Stage #2: 4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine With potassium carbonate In 4-methyl-2-pentanone for 1h; Reflux;
99%
4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl 4-bromobutanoate
1092777-14-4

(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl 4-bromobutanoate

(R/S)-bepotastine L-menthyl ester
1092777-15-5

(R/S)-bepotastine L-menthyl ester

Conditions
ConditionsYield
With potassium carbonate In acetone for 7h; Product distribution / selectivity; Heating / reflux;99%
With potassium carbonate In acetone for 7h; Reflux;99%
With potassium carbonate In acetone for 7h; Reflux;99%
4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

(S)-(-)-2-((4-chlorophenyl)(piperidin-4-yloxy)methyl)pyridine

(S)-(-)-2-((4-chlorophenyl)(piperidin-4-yloxy)methyl)pyridine

Conditions
ConditionsYield
Stage #1: 4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine With (-)-O,O′-dibenzoyl-L-tartaric acid monohydrate In acetic acid methyl ester
Stage #2: With L-Tartaric acid In ethanol
Stage #3: With sodium hydroxide In water
98.6%
With (S)-2-acetylamino-3-phenylpropanoic acid In ethyl acetate at 50 - 60℃;45.4%
With (S)-Mandelic acid In methanol at 60℃; for 2h; Reflux;42%
Multi-step reaction with 2 steps
1: ethyl acetate / 1 h / 65 °C / Large scale
2: hydrogenchloride / water / Large scale
View Scheme
4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

(S)-2-acetylamino-3-phenylpropanoic acid
2018-61-3

(S)-2-acetylamino-3-phenylpropanoic acid

(S)-2-[(4-chlorophenyl)(4-piperidinyloxy)methyl]pyridine N-acetyl-L-phenylalanine

(S)-2-[(4-chlorophenyl)(4-piperidinyloxy)methyl]pyridine N-acetyl-L-phenylalanine

Conditions
ConditionsYield
In ethyl acetate at 65℃; for 1h; Solvent; Temperature; Large scale;80%
4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

3,4-Diacetoxy-benzoesaeure
58534-64-8

3,4-Diacetoxy-benzoesaeure

(4-((4-chlorophenyl)(pyridin-2-yl)methoxy)piperidin-1-yl)(3,4-dihydroxyphenyl)methanone

(4-((4-chlorophenyl)(pyridin-2-yl)methoxy)piperidin-1-yl)(3,4-dihydroxyphenyl)methanone

Conditions
ConditionsYield
Stage #1: 3,4-Diacetoxy-benzoesaeure With phosphorus pentachloride In dichloromethane at 0 - 10℃; for 2h;
Stage #2: 4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine With triethylamine In dichloromethane at 0 - 20℃; for 2h;
78.1%
4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

2,5-dihydroxybenzoic acid.
490-79-9

2,5-dihydroxybenzoic acid.

(4-((4-chlorophenyl)(pyridin-2-yl)methoxy)piperidin-1-yl)(2,5-dihydroxyphenyl)methanone

(4-((4-chlorophenyl)(pyridin-2-yl)methoxy)piperidin-1-yl)(2,5-dihydroxyphenyl)methanone

Conditions
ConditionsYield
With benzotriazol-1-ol; 1,2-dichloro-ethane; triethylamine In N,N-dimethyl-formamide at 60 - 80℃; for 4h;54.9%
4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

(S)-1,1'-binaphthyl-2,2'-diyl hydrogen phosphate
35193-63-6, 35193-64-7, 39648-67-4, 50574-52-2

(S)-1,1'-binaphthyl-2,2'-diyl hydrogen phosphate

C17H19ClN2O*C20H13O4P

C17H19ClN2O*C20H13O4P

Conditions
ConditionsYield
In N,N-dimethyl-formamide; acetone at 45℃; for 0.166667h; Solvent; Temperature;40%
4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

3-methoxy-4-hydroxybenzoic acid
121-34-6

3-methoxy-4-hydroxybenzoic acid

4-((4-chlorophenyl)(pyridin-2-yl)methoxy)piperidin-1-yl(4-hydroxy-3-methoxyphenyl)methanone

4-((4-chlorophenyl)(pyridin-2-yl)methoxy)piperidin-1-yl(4-hydroxy-3-methoxyphenyl)methanone

Conditions
ConditionsYield
With benzotriazol-1-ol; 1,2-dichloro-ethane; triethylamine In N,N-dimethyl-formamide at 60 - 80℃; for 4h;31.6%
4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

2-bromoethanol
540-51-2

2-bromoethanol

2-[4-[(4-chlorophenyl)-pyridin-2-ylmethoxy]-1-piperidyl]ethanol
125602-93-9

2-[4-[(4-chlorophenyl)-pyridin-2-ylmethoxy]-1-piperidyl]ethanol

Conditions
ConditionsYield
With potassium carbonate In acetone0.64 g (56%)
4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

2-(2-bromoethyl)isoindoline-1,3-dione
574-98-1

2-(2-bromoethyl)isoindoline-1,3-dione

hydrazine hydrate
7803-57-8

hydrazine hydrate

2-[4-[(4-chlorophenyl)-pyridin-2-ylmethoxy]-1-piperidyl]ethylamine
125602-94-0

2-[4-[(4-chlorophenyl)-pyridin-2-ylmethoxy]-1-piperidyl]ethylamine

Conditions
ConditionsYield
With sodium hydroxide; potassium carbonate In 1,4-dioxane; ethanol3.50 g (41%)
4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

Ethyl 3-bromopropionate
539-74-2

Ethyl 3-bromopropionate

ethyl 3-[4-[(4-chlorophenyl)-pyridin-2-ylmethoxy]-1-piperidyl]propionate
125602-67-7

ethyl 3-[4-[(4-chlorophenyl)-pyridin-2-ylmethoxy]-1-piperidyl]propionate

Conditions
ConditionsYield
With potassium carbonate In 1,4-dioxane; methanol; chloroform1.78 g (67%)
4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

4-bromoethylbutanoate
2969-81-5

4-bromoethylbutanoate

4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidine-1-yl]butyric acid ethyl ester

4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidine-1-yl]butyric acid ethyl ester

Conditions
ConditionsYield
With potassium carbonate In methanol; chloroform; acetone6.26 g (91%)
4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

A

5-chloro-2-pentanone
5891-21-4

5-chloro-2-pentanone

B

5-[4-[(4-chlorophenyl)-pyridin-2-ylmethoxy]-1-piperidyl]-2-pentanone

5-[4-[(4-chlorophenyl)-pyridin-2-ylmethoxy]-1-piperidyl]-2-pentanone

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

A

propyl 4-[4-[(4-chlorophenyl)-pyridin-2-ylmethoxy]-1-piperidyl]butanoate

propyl 4-[4-[(4-chlorophenyl)-pyridin-2-ylmethoxy]-1-piperidyl]butanoate

B

4-chloro-butyric acid propyl ester
3153-35-3

4-chloro-butyric acid propyl ester

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

A

ethyl 4-[4-[(4-chlorophenyl)-pyridin-2-ylmethoxy]-1-piperidyl]-2-butenoate

ethyl 4-[4-[(4-chlorophenyl)-pyridin-2-ylmethoxy]-1-piperidyl]-2-butenoate

B

4-bromo-trans-crotonic acid ethyl ester
37746-78-4

4-bromo-trans-crotonic acid ethyl ester

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

A

4-[(4-chlorophenyl)-pyridin-2-ylmethoxy]-1-(3-benzoylpropyl)piperidine

4-[(4-chlorophenyl)-pyridin-2-ylmethoxy]-1-(3-benzoylpropyl)piperidine

B

4-chloro-1-phenylbutan-1-one
939-52-6

4-chloro-1-phenylbutan-1-one

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

A

4-[(4-chlorophenyl)-pyridin-2-ylmethoxy]-1-[3-(4-tert-butylbenzoyl)propyl]piperidine

4-[(4-chlorophenyl)-pyridin-2-ylmethoxy]-1-[3-(4-tert-butylbenzoyl)propyl]piperidine

B

4'-tert-butyl-4-chlorobutyrophenone
43076-61-5

4'-tert-butyl-4-chlorobutyrophenone

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

A

N,N-dimethyl-4-[4-[(4-chlorophenyl)-pyridin-2-ylmethoxy]-1-piperidyl]butanamide

N,N-dimethyl-4-[4-[(4-chlorophenyl)-pyridin-2-ylmethoxy]-1-piperidyl]butanamide

B

N,N-dimethyl-4-chlorobutyramide
22813-58-7

N,N-dimethyl-4-chlorobutyramide

2-((2-bromoethyl)thio)benzo[d]oxazole

2-((2-bromoethyl)thio)benzo[d]oxazole

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

2-[2-[4-[(4-Chlorophenyl)-pyridin-2-ylmethoxy]-1-piperidyl]-ethylthio]benzoxazole

2-[2-[4-[(4-Chlorophenyl)-pyridin-2-ylmethoxy]-1-piperidyl]-ethylthio]benzoxazole

Conditions
ConditionsYield
With potassium carbonate In 1,4-dioxane1.51 g (84%)
2-(2-bromoethylthio)-5-chlorobenzoxazole

2-(2-bromoethylthio)-5-chlorobenzoxazole

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

5-chloro-2-[2-[4-[(4-chlorophenyl)-pyridin-2-ylmethoxy]-1-piperidyl]ethylthio]benzoxazole

5-chloro-2-[2-[4-[(4-chlorophenyl)-pyridin-2-ylmethoxy]-1-piperidyl]ethylthio]benzoxazole

Conditions
ConditionsYield
With potassium carbonate In 1,4-dioxane; methanol; chloroform1.83 g (54%)
2-(2-bromoethylthio)-6-methylbenzoxazole

2-(2-bromoethylthio)-6-methylbenzoxazole

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

2-[2-[4-[(4-Chlorophenyl)-pyridin-2-ylmethoxy]-1-piperidyl]-ethylthio]-6-methylbenzoxazole

2-[2-[4-[(4-Chlorophenyl)-pyridin-2-ylmethoxy]-1-piperidyl]-ethylthio]-6-methylbenzoxazole

Conditions
ConditionsYield
With potassium carbonate In methanol; chloroform; acetone1.55 g (91%)
2-(2-chloroethylthio)benzoxazole

2-(2-chloroethylthio)benzoxazole

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

2-[2-[4-[(4-Chlorophenyl)-pyridin-2-ylmethoxy]-1-piperidyl]-ethylthio]benzothiazole

2-[2-[4-[(4-Chlorophenyl)-pyridin-2-ylmethoxy]-1-piperidyl]-ethylthio]benzothiazole

Conditions
ConditionsYield
With potassium carbonate In 1,4-dioxane0.52 g (20%)
4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine
122368-54-1

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

2-((3-bromopropyl)thio)benzo[d]thiazole
125603-00-1

2-((3-bromopropyl)thio)benzo[d]thiazole

2-[3-[4-[(4-Chlorophenyl)-pyridin-2-ylmethoxy]-1-piperidyl]-propylthio]benzothiazole

2-[3-[4-[(4-Chlorophenyl)-pyridin-2-ylmethoxy]-1-piperidyl]-propylthio]benzothiazole

Conditions
ConditionsYield
With potassium carbonate In methanol; chloroform; acetone0.52 g (41%)

122368-54-1Relevant articles and documents

Synthesis, characterization and in vitro evaluation of novel enantiomerically-pure sulphonamide antimalarials

Anusha, Sebastian,Sinha, Ameya,Babu Rajeev,Chu, Trang T. T.,Mathai, Jessin,Ximei, Huang,Fuchs, Julian E.,Shivananju, Nanjundaswamy,Bender, Andreas,Preiser, Peter Rainer,Rangappa, Kanchugarakoppal S.,Basappa,Chandramohanadas, Rajesh

, p. 10681 - 10690 (2015)

Malaria parasites are currently gaining drug-resistance rapidly, across countries and continents. Hence, the discovery and development of novel chemical scaffolds, with superior antimalarial activity remain an important priority, for the developing world. Our report describes the development, characterization and evaluation of novel bepotastine-based sulphonamide antimalarials inhibiting asexual stage development of Plasmodium falciparum parasites in vitro. The screening results showed potent inhibitory activity of a number of novel sulphonamides against P. falciparum at low micromolar concentrations, in particular in late-stage parasite development. Based on computational studies we hypothesize N-myristoyltransferase as the target of the compounds developed here. Our results demonstrate the value of novel bepotastine-based sulphonamide compounds for targeting the asexual developmental stages of P. falciparum.

Light-induced metal-free transformations of unactivated pyridotriazoles

Zhang, Ziyan,Yadagiri, Dongari,Gevorgyan, Vladimir

, p. 8399 - 8404 (2019/09/30)

A highly efficient and practical method for incorporation of the arylmethylpyridyl moiety into diverse molecules has been developed. This method features the transition metal-free light-induced room temperature transformation of pyridotriazoles into pyridyl carbenes, which are capable of smooth arylation, X-H insertion, and cyclopropanation reactions. The synthetic usefulness of the developed method was illustrated in a facile synthesis of biologically active molecules.

METHOD OF SYNTHESIZING BEPOTASTINE OR BENZENESULFONIC ACID SALT THEREOF AND INTERMEDIATES USED THEREIN

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, (2014/03/21)

The present invention relates to a novel method of synthesizing bepotastine or its benzenesulfonic acid salt and novel intermediates used therein. The present invention uses L-α-hydroxy acid for chiral resolution to form an L-α-hydroxy acid salt of a compound represented by the following formula (VII-1), so as to synthesize bepotastine or its benzenesulfonic acid salt in high optical purity.

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