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83881-52-1

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83881-52-1 Usage

Description

Different sources of media describe the Description of 83881-52-1 differently. You can refer to the following data:
1. Cetirizine hydrochloride is an orally-active and selective histamine (H1)-receptor antagonist. It is a second-generation antihistamine and a human metabolite of hydroxyzine. Three important features of cetirizine are: a high specificity fort he H1-receptor; a low need for metabolism, and the existence of non-H1-dependent activities on cells involved in the pathogenesis of allergy. Cetirizine is used to treat seasonal allergic rhinitis (SAR), perennial allergic rhinitis, useful in treating urticaria and atopic dermatitis. Cetirizine possesses also mild anti-inflammatory effects.
2. Cetirizine hydrochloride is a once-daily, non-sedating antihistamine useful in the treatment of allergic rhinitis, urticaria and conjunctivitis. It is reported to be more effective than most other agents in this category such as terfenadine and astemizole.

References

[1] E. J. Corey and Christopher J. Helal, Catalytic Enantioselective Synthesis of the Second-Generation Histamine Antagonist Cetirizine Hydrochloride, Tetrahedron Letters, 1996, vol. 37, 4837-4840 [2] Jay M. Portnoy and Chitra Dinakar, Review of cetirizine hydrochloride for the treatment of allergic disorders, Journal of Expert Opinion on Pharmacotherapy, 2004, vol. 5, 125-135

Chemical Properties

Cetirizine Hydrochloride occurs as a white crystalline powder or crystalline solid. It is very soluble in water, and slightly soluble in ethanol (99.5). It dissolves in 0.1 mol/L hydrochloric acid TS. A solution of Cetirizine Hydrochloride (1 in 10) shows no optical rotation.

Originator

UCB (Belgium)

Uses

Cetirizine hydrochloride is a nonsedating type histamine H1-receptor antagonist. A major metabolite of Hydroxyzine. Pharmacological activity resides primarily in the (R)-isomer. It is Cetirizine is an antihistamine medicine that is effective in the treatment of allergic rhinitis, chronic urticaria, and pollen-induced asthma. Unlike many traditional antihistamines, it does not cause drowsiness or anticholinergic side effects.

Application

Cetirizine Hydrochloride may be used as a pharmaceutical reference standard for the determination of the analyte in pharmaceutical formulations by various chromatography techniques.

Indications

Cetirizine HCl (Zyrtec) is the carboxylic acid metabolite of hydroxyzine. It is a selective, peripheral H1 receptor antagonist. It is a long-lasting antihistamine. It does not appear to have the same adverse cardiac effects as the other nonsedating H1 antihistamines; however, additional data are required. Indicated for allergic rhinitis and chronic urticaria.

Definition

ChEBI: Cetirizine hydrochloride is a diarylmethane.

Manufacturing Process

Preparation of 2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]- ethoxy]acetic acid (cetirizine). To a mixture of 50 g 2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]- ethanol and 225 ml of tert-butanol at 45°C under a nitrogen was added 21 g tert-BuOK. The temperature was raised to 75-80°C and the mixture was kept at this temperature. After 45 min was added 11 g sodium chloracetate; after 1.5 hour was added 5.2 g tert-BuOK; after 2 hours was added 5.64 g sodium chloracetate; after 2.5 hours was added 1.9 g tert-BuOK; after 3 hours was added 1.9 g sodium chloracetate; after 3.5 hours was added 0.8 g tert-BuOK; and after 4 hours was added 1.13 g sodium chloracetate. Then about 150 ml tert-butanol was distilled of, 190 ml of water was added and the distillation of tert-butanol was continued until the temperature of the vapour reaches 100°C. To the reaction mixture was added 60 ml of water and 8 ml concentrated hydrochloric acid to pH 8. Unreacted 2-[4-[(4-chlorophenyl) phenylmethyl]-1-piperazinyl]-ethanol was extracted with diethyl ether. The aqueous phase was acidified to pH 5 by addition of hydrochloric acid and extracted with dichloromethane (200 ml x 3). The extract was dried over MgSO4, filtered and concentrated in a rotary evaporator. An obtained oil was allowed to crystallize by addition of 150 ml of 2-butanone, yields of 2-[4-[(4- chlorophenyl)phenylmethyl]-1-piperazinyl]-ethoxy]acetic acid 55.5%, M.P. 146-148°C. 32.7 g 2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]-ethoxy]acetic acid was suspended in a mixture of 125 ml of water and 13.8 ml 37% aqueous hydrochloric acid. The mixture was concentrated in a rotary evaporator. An obtained oil was allowed to crystallize by addition of 245 ml of 2-butanone, yields of 2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]-ethoxy]acetic acid dihydrochloride 88%, M.P. 228.22°C.

Therapeutic Function

Antihistaminic; Antiallergic

General Description

Cetirizine hydrochloride, a second generation antihistaminic drug, is one of the carboxylated metabolites of hydroxyzine that can typically bind to histamine H1 receptor. It is effective against diseases such as urticaria, angioedema, allergies and hay fever.

Biological Activity

Histamine H 1 receptor antagonist that displays selectivity over other receptors at concentrations up to 10 μ M. A non-sedating antihistamine that inhibits histamine release and eosinophil chemotaxis during secondary phase allergic response. Inhibits activation of eosinophils, neutrophils and monocytes in vivo .

Biochem/physiol Actions

Cetirizine hydrochloride is an orally active and selective H1-receptor antagonist. Antihistaminic; Piperazines. Non-sedating type histamine H1-receptor antagonist; major metabolite of hydroxyzine. Pharmacological activity resides primarily in the (R)-isomer.

Veterinary Drugs and Treatments

Cetirizine is a H1 receptor blocking antihistamine agent that may be useful for the adjunctive treatment of histamine-mediated pruritic conditions in dogs or cats.

Drug interactions

Potentially hazardous interactions with other drugs Antivirals: concentration possibly increased by ritonavir.

Metabolism

Cetirizine does not undergo extensive first pass metabolism. About two thirds of the dose is excreted unchanged in urine.

Dosage forms

5 to 10mg daily.

Check Digit Verification of cas no

The CAS Registry Mumber 83881-52-1 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 8,3,8,8 and 1 respectively; the second part has 2 digits, 5 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 83881-52:
(7*8)+(6*3)+(5*8)+(4*8)+(3*1)+(2*5)+(1*2)=161
161 % 10 = 1
So 83881-52-1 is a valid CAS Registry Number.
InChI:InChI=1/C21H25ClN2O3.2ClH/c22-19-8-6-18(7-9-19)21(17-4-2-1-3-5-17)24-12-10-23(11-13-24)14-15-27-16-20(25)26;;/h1-9,21H,10-16H2,(H,25,26);2*1H

83881-52-1 Well-known Company Product Price

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  • (Code)Product description
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  • TCI America

  • (C2316)  Cetirizine Dihydrochloride  >98.0%(HPLC)(T)

  • 83881-52-1

  • 5g

  • 910.00CNY

  • Detail
  • TCI America

  • (C2316)  Cetirizine Dihydrochloride  >98.0%(HPLC)(T)

  • 83881-52-1

  • 25g

  • 2,900.00CNY

  • Detail
  • Sigma-Aldrich

  • (C0980650)  Cetirizinedihydrochloride  European Pharmacopoeia (EP) Reference Standard

  • 83881-52-1

  • C0980650

  • 1,880.19CNY

  • Detail
  • Sigma-Aldrich

  • (Y0001197)  Cetirizine for peak identification  European Pharmacopoeia (EP) Reference Standard

  • 83881-52-1

  • Y0001197

  • 1,880.19CNY

  • Detail
  • USP

  • (1102929)  Cetirizinedihydrochloride  United States Pharmacopeia (USP) Reference Standard

  • 83881-52-1

  • 1102929-250MG

  • 4,588.74CNY

  • Detail

83881-52-1SDS

SAFETY DATA SHEETS

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

Version: 1.0

Creation Date: Aug 12, 2017

Revision Date: Aug 12, 2017

1.Identification

1.1 GHS Product identifier

Product name Cetirizine Dihydrochloride

1.2 Other means of identification

Product number -
Other names 2-[2-[4-[(4-chlorophenyl)-phenylmethyl]piperazin-1-yl]ethoxy]acetic acid,dihydrochloride

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:83881-52-1 SDS

83881-52-1Synthetic route

cetirizine
83881-51-0

cetirizine

cetirizine dihydrochloride
83881-52-1

cetirizine dihydrochloride

Conditions
ConditionsYield
With hydrogenchloride In water; acetone at 20 - 50℃; for 2h;87.9%
With hydrogenchloride In water pH=8;
With hydrogenchloride In ethyl acetate; isopropyl alcohol at 25 - 35℃; for 1 - 2h; pH=2;
2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethan-1-ol
109806-71-5

2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethan-1-ol

sodium monochloroacetic acid
3926-62-3

sodium monochloroacetic acid

cetirizine dihydrochloride
83881-52-1

cetirizine dihydrochloride

Conditions
ConditionsYield
Stage #1: 2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethan-1-ol; sodium monochloroacetic acid With sodium hydroxide In water; dimethyl sulfoxide; toluene at 30 - 35℃; for 14 - 18h;
Stage #2: With hydrogenchloride In water; acetone at 20℃;
87.4%
C21H25ClN2O2
770697-99-9

C21H25ClN2O2

cetirizine dihydrochloride
83881-52-1

cetirizine dihydrochloride

Conditions
ConditionsYield
Stage #1: C21H25ClN2O2 With potassium dihydrogenphosphate; phosphoric acid; dihydrogen peroxide In dichloromethane; dimethyl sulfoxide at 5 - 25℃; for 8h; pH=4 - 5;
Stage #2: With hydrogenchloride In butanone at 60℃;
86%
2-(2-(4-((4-chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)acetamide
83881-37-2, 163837-41-0, 163837-43-2

2-(2-(4-((4-chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)acetamide

cetirizine dihydrochloride
83881-52-1

cetirizine dihydrochloride

Conditions
ConditionsYield
Stage #1: 2-(2-(4-((4-chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)acetamide With sodium hydroxide In water Heating / reflux;
Stage #2: With hydrogenchloride In ethyl acetate; isopropyl alcohol for 1 - 2h;
cetirizine hydrochloride
83881-51-0

cetirizine hydrochloride

cetirizine dihydrochloride
83881-52-1

cetirizine dihydrochloride

Conditions
ConditionsYield
With hydrogenchloride In ethyl acetate; isopropyl alcohol at 25 - 35℃; for 1.16667 - 2.25h; pH=2;
2-(2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)-N,N-dimethylacetamide dihydrochloride

2-(2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)-N,N-dimethylacetamide dihydrochloride

cetirizine dihydrochloride
83881-52-1

cetirizine dihydrochloride

Conditions
ConditionsYield
With hydrogenchloride; sodium hydroxide In dichloromethane; water; acetone
With water; sodium hydroxide for 3h; Reflux; Large scale reaction;
(RS)-N,N-diethyl-{2-[4-(α-phenyl-p-chloro-benzyl)piperazin-1-yl]ethoxy}-acetamide
343781-29-3

(RS)-N,N-diethyl-{2-[4-(α-phenyl-p-chloro-benzyl)piperazin-1-yl]ethoxy}-acetamide

cetirizine dihydrochloride
83881-52-1

cetirizine dihydrochloride

Conditions
ConditionsYield
In 1,4-dioxane
(RS)-N,N-diallyl-{2-[4-(α-phenyl-p-chloro-benzyl)piperazin-1-yl]ethoxy}-acetamide
343781-30-6

(RS)-N,N-diallyl-{2-[4-(α-phenyl-p-chloro-benzyl)piperazin-1-yl]ethoxy}-acetamide

cetirizine dihydrochloride
83881-52-1

cetirizine dihydrochloride

Conditions
ConditionsYield
In 1,4-dioxane
(+/-)-{2-[4-(α-phenyl-p-chlorobenzyl)-piperazin-1-yl]-ethoxy}-acetic acid-N,N-dimethylamide
940980-27-8, 940980-28-9, 343781-27-1

(+/-)-{2-[4-(α-phenyl-p-chlorobenzyl)-piperazin-1-yl]-ethoxy}-acetic acid-N,N-dimethylamide

cetirizine dihydrochloride
83881-52-1

cetirizine dihydrochloride

methyl tert-butylether

methyl tert-butylether

tert-butyl 2-(2-chloroethoxy)acetate

tert-butyl 2-(2-chloroethoxy)acetate

N-(4-chlorobenzhydryl)piperazine
303-26-4

N-(4-chlorobenzhydryl)piperazine

pyrographite
7440-44-0

pyrographite

cetirizine dihydrochloride
83881-52-1

cetirizine dihydrochloride

Conditions
ConditionsYield
With ammonium hydroxide; sodium hydroxide; sodium carbonate In N-methyl-acetamide; hydrogenchloride; acetone
2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethan-1-ol dihydrochloride

2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethan-1-ol dihydrochloride

cetirizine dihydrochloride
83881-52-1

cetirizine dihydrochloride

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1.1: water / toluene
2.1: sodium methylate / toluene / 10 - 15 °C / Inert atmosphere; Large scale reaction
2.2: 2 h / 50 - 60 °C / Large scale reaction
3.1: water; sodium hydroxide / 3 h / Reflux; Large scale reaction
View Scheme
(4-chlorophenyl)phenylmethanol
119-56-2

(4-chlorophenyl)phenylmethanol

cetirizine dihydrochloride
83881-52-1

cetirizine dihydrochloride

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1.1: thionyl chloride / toluene / 1 h / 85 - 90 °C / Large scale reaction
2.1: toluene / 3 h / 80 °C / Large scale reaction
2.2: pH 1 / Large scale reaction
3.1: water / toluene
4.1: sodium methylate / toluene / 10 - 15 °C / Inert atmosphere; Large scale reaction
4.2: 2 h / 50 - 60 °C / Large scale reaction
5.1: water; sodium hydroxide / 3 h / Reflux; Large scale reaction
View Scheme
1-chloro-4-(chloro(phenyl)methyl)benzene
134-83-8

1-chloro-4-(chloro(phenyl)methyl)benzene

cetirizine dihydrochloride
83881-52-1

cetirizine dihydrochloride

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1.1: toluene / 3 h / 80 °C / Large scale reaction
1.2: pH 1 / Large scale reaction
2.1: water / toluene
3.1: sodium methylate / toluene / 10 - 15 °C / Inert atmosphere; Large scale reaction
3.2: 2 h / 50 - 60 °C / Large scale reaction
4.1: water; sodium hydroxide / 3 h / Reflux; Large scale reaction
View Scheme
2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethan-1-ol
109806-71-5

2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethan-1-ol

cetirizine dihydrochloride
83881-52-1

cetirizine dihydrochloride

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1.1: sodium methylate / toluene / 10 - 15 °C / Inert atmosphere; Large scale reaction
1.2: 2 h / 50 - 60 °C / Large scale reaction
2.1: water; sodium hydroxide / 3 h / Reflux; Large scale reaction
View Scheme
4-chlorobenzophenone
134-85-0

4-chlorobenzophenone

cetirizine dihydrochloride
83881-52-1

cetirizine dihydrochloride

Conditions
ConditionsYield
Multi-step reaction with 6 steps
1.1: water; Aliquat 336 / toluene / 20 °C / Large scale reaction
1.2: 5 h / 50 °C / Large scale reaction
2.1: thionyl chloride / toluene / 1 h / 85 - 90 °C / Large scale reaction
3.1: toluene / 3 h / 80 °C / Large scale reaction
3.2: pH 1 / Large scale reaction
4.1: water / toluene
5.1: sodium methylate / toluene / 10 - 15 °C / Inert atmosphere; Large scale reaction
5.2: 2 h / 50 - 60 °C / Large scale reaction
6.1: water; sodium hydroxide / 3 h / Reflux; Large scale reaction
View Scheme
cetirizine dihydrochloride
83881-52-1

cetirizine dihydrochloride

diazomethyl-trimethyl-silane
18107-18-1

diazomethyl-trimethyl-silane

(2-{4-[(4-chlorophenyl)phenylmethyl]piperazin-1-yl}ethoxy)acetic acid methyl ester dihydrochloride

(2-{4-[(4-chlorophenyl)phenylmethyl]piperazin-1-yl}ethoxy)acetic acid methyl ester dihydrochloride

Conditions
ConditionsYield
In methanol for 2h; Reflux;99%
cetirizine dihydrochloride
83881-52-1

cetirizine dihydrochloride

diazomethyl-trimethyl-silane
18107-18-1

diazomethyl-trimethyl-silane

methyl 2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-acetate
83881-46-3, 163837-44-3, 163837-46-5

methyl 2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-acetate

Conditions
ConditionsYield
In methanol; hexane at 0℃; for 0.166667h;97%
cetirizine dihydrochloride
83881-52-1

cetirizine dihydrochloride

methyl 2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-acetate
83881-46-3, 163837-44-3, 163837-46-5

methyl 2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-acetate

Conditions
ConditionsYield
With sulfuric acid In methanol for 10h; Heating / reflux;95%
cetirizine dihydrochloride
83881-52-1

cetirizine dihydrochloride

(2-{4-[(4-chlorophenyl)phenylmethyl]piperazin-1-yl}ethoxy)acetyl chloride dihydrochloride

(2-{4-[(4-chlorophenyl)phenylmethyl]piperazin-1-yl}ethoxy)acetyl chloride dihydrochloride

Conditions
ConditionsYield
Stage #1: cetirizine dihydrochloride With thionyl chloride In N,N-dimethyl-formamide for 3h;
Stage #2: In N,N-dimethyl-formamide; toluene for 1h;
92%
Diazoethan
1117-96-0

Diazoethan

cetirizine dihydrochloride
83881-52-1

cetirizine dihydrochloride

(2-{4-[(4-chlorophenyl)phenylmethyl]piperazin-1-yl}ethoxy)acetic acid ethyl ester

(2-{4-[(4-chlorophenyl)phenylmethyl]piperazin-1-yl}ethoxy)acetic acid ethyl ester

Conditions
ConditionsYield
In tetrahydrofuran at 0℃;90%
vanadium(IV) fluoride
10049-16-8

vanadium(IV) fluoride

cetirizine dihydrochloride
83881-52-1

cetirizine dihydrochloride

difluorovanadium(IV)(2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy acetate)
1080673-10-4

difluorovanadium(IV)(2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy acetate)

Conditions
ConditionsYield
In methanol methanolic soln. of VF4 added to methanolic soln. of C21H25O3N2Cl dropwise with stirring, mixt. had pH 3, refluxed for 2 h, kept overnight with stirring at room temp.; solvent removed on a rotary apparatus under reduced pressure; recrystn. (MeOH/n-hexane, 1/1); elem. anal.;82%
1-hydroxy-pyrrolidine-2,5-dione
6066-82-6

1-hydroxy-pyrrolidine-2,5-dione

2-methoxyethylamine
109-85-3

2-methoxyethylamine

cetirizine dihydrochloride
83881-52-1

cetirizine dihydrochloride

mPEG1-cetirizine
1059587-86-8

mPEG1-cetirizine

Conditions
ConditionsYield
Stage #1: 1-hydroxy-pyrrolidine-2,5-dione; cetirizine dihydrochloride With dicyclohexyl-carbodiimide In N,N-dimethyl-formamide at 20℃;
Stage #2: 2-methoxyethylamine In N,N-dimethyl-formamide for 5h;
80%
cetirizine dihydrochloride
83881-52-1

cetirizine dihydrochloride

2-(2-(4-((4-chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)acetamide
83881-37-2, 163837-41-0, 163837-43-2

2-(2-(4-((4-chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)acetamide

Conditions
ConditionsYield
Stage #1: cetirizine dihydrochloride With thionyl chloride In N,N-dimethyl-formamide at 20℃; for 3h; Large scale;
Stage #2: With ammonia In N,N-dimethyl-formamide; toluene at 0 - 30℃; Large scale;
78.5%
Multi-step reaction with 2 steps
1: methanol / 2 h / Reflux
2: ammonia / methanol / 775.74 - 1551.49 Torr
View Scheme
copper(II) chloride hexahydrate

copper(II) chloride hexahydrate

L-alanin
56-41-7

L-alanin

cetirizine dihydrochloride
83881-52-1

cetirizine dihydrochloride

[Cu(CTZ)(Ala)(H2O)]

[Cu(CTZ)(Ala)(H2O)]

Conditions
ConditionsYield
With sodium hydrogencarbonate In ethanol at 90℃;77%
nickel(II) chloride hexahydrate

nickel(II) chloride hexahydrate

L-alanin
56-41-7

L-alanin

cetirizine dihydrochloride
83881-52-1

cetirizine dihydrochloride

[Ni(CTZ)(Ala)(H2O)]

[Ni(CTZ)(Ala)(H2O)]

Conditions
ConditionsYield
With sodium hydrogencarbonate In ethanol at 90℃;72%
cobalt(II) chloride hexahydrate

cobalt(II) chloride hexahydrate

L-alanin
56-41-7

L-alanin

cetirizine dihydrochloride
83881-52-1

cetirizine dihydrochloride

[Co(CTZ)(Ala)(H2O)]·H2O

[Co(CTZ)(Ala)(H2O)]·H2O

Conditions
ConditionsYield
With sodium hydrogencarbonate In ethanol at 90℃;65%
(Z)-4-hydroxybut-2-enyl 1-(nitrooxy)ethyl carbonate
1345092-28-5

(Z)-4-hydroxybut-2-enyl 1-(nitrooxy)ethyl carbonate

cetirizine dihydrochloride
83881-52-1

cetirizine dihydrochloride

(Z)-4-((1-(nitrooxy)ethoxy)carbonyloxy)but-2-enyl 2-(2-(4-((4-chlorophenyl) (phenyl)methyl)piperazin-1-yl)ethoxy)acetate
1345091-84-0

(Z)-4-((1-(nitrooxy)ethoxy)carbonyloxy)but-2-enyl 2-(2-(4-((4-chlorophenyl) (phenyl)methyl)piperazin-1-yl)ethoxy)acetate

Conditions
ConditionsYield
With dmap; triethylamine; dicyclohexyl-carbodiimide In dichloromethane for 2h;32.6%
bis(2-hydroxyethyl) disulfide
1892-29-1

bis(2-hydroxyethyl) disulfide

cetirizine dihydrochloride
83881-52-1

cetirizine dihydrochloride

C25H33ClN2O4S2

C25H33ClN2O4S2

Conditions
ConditionsYield
With triethylamine; dicyclohexyl-carbodiimide; dmap In dichloromethane at 20℃; for 15h;19%
3-Hydroxybutyric acid
300-85-6, 625-71-8

3-Hydroxybutyric acid

cetirizine dihydrochloride
83881-52-1

cetirizine dihydrochloride

C25H31ClN2O5

C25H31ClN2O5

Conditions
ConditionsYield
Stage #1: 3-Hydroxybutyric acid; cetirizine dihydrochloride With 1-hydroxy-pyrrolidine-2,5-dione; N-ethyl-N,N-diisopropylamine In dichloromethane; N,N-dimethyl-formamide for 15h;
Stage #2: With 1,1,1,3',3',3'-hexafluoro-propanol In dichloromethane for 0.166667h;
2%
cetirizine dihydrochloride
83881-52-1

cetirizine dihydrochloride

cetirizine
83881-51-0

cetirizine

Conditions
ConditionsYield
With sodium hydroxide In water for 4.7h;
cetirizine dihydrochloride
83881-52-1

cetirizine dihydrochloride

cetirizine hydrochloride
83881-51-0

cetirizine hydrochloride

Conditions
ConditionsYield
Stage #1: cetirizine dihydrochloride With sodium hydroxide In water pH=12;
Stage #2: With hydrogenchloride In water pH=2 - 3;

83881-52-1Relevant articles and documents

A synthesis process of cetirizine hydrochloride

-

Paragraph 0074; 0075; 0076; 0077, (2017/03/08)

A new technology for synthesizing cetirizine hydrochloride. The technology includes following steps: oxidizing hydroxyzine, which is used as a raw material, into a substance containing an aldehyde group; further oxidizing the substance containing the aldehyde group into cetirizine; and finally performing a salification and purification process to obtain the cetirizine hydrochloride. A total yield of the synthetic method is higher than 80%. Meanwhile, the method is simple in operation, is short in production period, is low in energy consumption and cost, is little in waste water, waste gas and residues and is suitable for large-scale industrial production.

Process for obtaining cetirizine dihydrochloride

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Page/Page column 3-4, (2009/02/11)

Process for the synthesis of cetirizine dihydrochloride, wherein (a) a solution of {2-[4-(α-phenyl-p-chlorobenzyl)piperazin-1-yl]}ethanol in 1-7 volumes, referred to the weight of {2-[4-(α-phenyl-p-chlorobenzyl)piperazin-1-yl]}ethanol, of an organic solvent having a boiling point higher than 90° C. and being chosen from the group consisting of aliphatic, cycloalifatic or aromatic solvents is provided, whereafter(b) per equivalent of {2-[4-(α-phenyl-p-chlorobenzyl)piperazin-1-yl]}ethanol employed, 1-2 equivalents of a metal haloacetate or of haloacetic acid, as well as 3-7 equivalents of an alkaly metal hydroxyde are added to the solution as per (a), providing a reaction mixture, where 0.05-0.3 volumes, referred to the weight of {2-[4-(α-phenyl-p-chlorobenzyl)piperazin-1-yl]}ethanol employed, of water and 0.1-1.2 volumes, referred to the weight of {2-[4-(α-phenyl-p-chlorobenzyl)piperazin-1-yl]}ethanol employed, of a polar aprotic, water miscible solvent are added, keeping the internal temperature of the reaction mixture below 60° C., whereafter(c) the cetirizine base formed within the reaction mixture is converted into its dihydrochloride salt and isolated as such.

Novel amorphous form of [2-[4-[(4-chlorophenyl)-phenyl methyl]-1-piperazinyl]ethoxy]acetic acid and process for the preparation thereof

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Page/Page column 6, (2008/06/13)

A novel amorphous form of cetirizine and processes for making the amorphous form as well as compositions, pharmaceutical compositions, and methods utilizing the crystalline form are described.

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