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121-30-2

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  • China Biggest factory Supply High Quality 4-Amino-6-chlorobenzene-1,3-disulfonamideCAS 121-30-2

    Cas No: 121-30-2

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121-30-2 Usage

Chemical Properties

Light Brown Solid

Uses

Different sources of media describe the Uses of 121-30-2 differently. You can refer to the following data:
1. Diuretic.
2. 4-Amino-6-chloro-1,3-benzenedisulfonamide was used in the synthesis of deuterated thiazides by undergoing condensation with appropriately labeled aldehydes.

General Description

Pharmaceutical secondary standards for application in quality control, provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to the preparation of in-house working standards.

Check Digit Verification of cas no

The CAS Registry Mumber 121-30-2 includes 6 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 3 digits, 1,2 and 1 respectively; the second part has 2 digits, 3 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 121-30:
(5*1)+(4*2)+(3*1)+(2*3)+(1*0)=22
22 % 10 = 2
So 121-30-2 is a valid CAS Registry Number.
InChI:InChI=1/C6H8ClN3O4S2/c7-3-1-4(8)6(16(10,13)14)2-5(3)15(9,11)12/h1-2H,8H2,(H2,9,11,12)(H2,10,13,14)

121-30-2 Well-known Company Product Price

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  • Sigma-Aldrich

  • (PHR1192)  4-Amino-6-chloro-1,3-benzendisulfonamide  pharmaceutical secondary standard; traceable to USP

  • 121-30-2

  • PHR1192-500MG

  • 1,024.57CNY

  • Detail
  • USP

  • (1057507)  BenzothiadiazineRelatedCompoundA  United States Pharmacopeia (USP) Reference Standard

  • 121-30-2

  • 1057507-100MG

  • 14,578.20CNY

  • Detail
  • Aldrich

  • (308560)  4-Amino-6-chloro-1,3-benzenedisulfonamide  98%

  • 121-30-2

  • 308560-5G

  • 484.38CNY

  • Detail
  • Aldrich

  • (308560)  4-Amino-6-chloro-1,3-benzenedisulfonamide  98%

  • 121-30-2

  • 308560-100G

  • 1,291.68CNY

  • Detail

121-30-2SDS

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 4-Amino-6-chlorobenzene-1,3-disulfonamide

1.2 Other means of identification

Product number -
Other names Salmid

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:121-30-2 SDS

121-30-2Synthetic route

4-amino-6-chloro-benzene-1,3-disulfonyl chloride
671-89-6

4-amino-6-chloro-benzene-1,3-disulfonyl chloride

chloraminophenamide
121-30-2

chloraminophenamide

Conditions
ConditionsYield
With ammonia
Conditions
ConditionsYield
With water at 37℃; phosphate buffer (pH: 7.4); or with human serum albumin;
With water at 37℃; Rate constant; phosphate buffer (pH: 7.4); or with human serum albumin;
Conditions
ConditionsYield
With water at 37℃; phosphate buffer (pH: 7.4); or with human serum albumin;
With water at 37℃; Rate constant; phosphate buffer (pH: 7.4); or with human serum albumin;
methanol
67-56-1

methanol

6-chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide
58-93-5

6-chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide

A

chloraminophenamide
121-30-2

chloraminophenamide

B

4-amino-1,3-benzenedisulfonamide
40642-90-8

4-amino-1,3-benzenedisulfonamide

C

4-Amino-6-hydroxy-benzene-1,3-disulfonic acid diamide

4-Amino-6-hydroxy-benzene-1,3-disulfonic acid diamide

D

6-Hydroxy-1,1-dioxo-1,2,3,4-tetrahydro-1λ6-benzo[1,2,4]thiadiazine-7-sulfonic acid amide

6-Hydroxy-1,1-dioxo-1,2,3,4-tetrahydro-1λ6-benzo[1,2,4]thiadiazine-7-sulfonic acid amide

E

3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide
23141-82-4

3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide

F

6-methoxy-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide
32059-40-8

6-methoxy-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide

Conditions
ConditionsYield
In water Product distribution; Mechanism; Irradiation; multistep reaction, photholytic decomposition; also in pure MeOH; effect of O2;
6-chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide
58-93-5

6-chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide

chloraminophenamide
121-30-2

chloraminophenamide

Conditions
ConditionsYield
In methanol for 2160h; Product distribution; Ambient temperature; stability study; further temperature, further solvent;
With sodium hydroxide at 95℃; for 1h;
With sodium hydroxide at 80℃; for 3.5h;
With hydrogenchloride In methanol; propan-1-ol; water for 80h; Kinetics;
6-chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide
58-93-5

6-chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide

A

chloraminophenamide
121-30-2

chloraminophenamide

B

formaldehyd
50-00-0

formaldehyd

Conditions
ConditionsYield
In ethanol at 90℃; for 528h; Equilibrium constant; Kinetics; Thermodynamic data; other temperature and time;
trichloromethiazide
133-67-5

trichloromethiazide

chloraminophenamide
121-30-2

chloraminophenamide

Conditions
ConditionsYield
pyrographite hydrolysis of benzothiadiazines;
pyrographite hydrolysis;
With water In ethanol at 35℃; Kinetics; Temperature; Solvent; pH-value; Concentration;
Conditions
ConditionsYield
In water at 60℃; for 336000h; pH=5.2; Substitution;
chloraminophenamide
121-30-2

chloraminophenamide

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: water / 37 °C / phosphate buffer (pH: 7.4); or with human serum albumin
2: water / 37 °C / phosphate buffer (pH: 7.4); or with human serum albumin
View Scheme
3-chloro-aniline
108-42-9

3-chloro-aniline

chloraminophenamide
121-30-2

chloraminophenamide

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: ClSO3H
2: NH3
View Scheme
Multi-step reaction with 2 steps
1: ClSO3H, NaCl / 150 °C
2: NH3
View Scheme
6-chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide
58-93-5

6-chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide

A

chloraminophenamide
121-30-2

chloraminophenamide

B

6-chloro-2-oxo-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide

6-chloro-2-oxo-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide

Conditions
ConditionsYield
With dihydrogen peroxide at 80℃; for 2h;
chloraminophenamide
121-30-2

chloraminophenamide

methyl 3,3-dimethoxypropionate
7424-91-1

methyl 3,3-dimethoxypropionate

2H-1,2,4-benzothiadiazine-7-(aminosulfonyl)-6-chloro-3,4-dihydro-1,1-dioxide-3-acetic acid methyl ester

2H-1,2,4-benzothiadiazine-7-(aminosulfonyl)-6-chloro-3,4-dihydro-1,1-dioxide-3-acetic acid methyl ester

Conditions
ConditionsYield
With hydrogenchloride In 1,4-dioxane; water at 40 - 90℃; for 0.5h;100%
chloraminophenamide
121-30-2

chloraminophenamide

1-bromo-2,2-dimethoxyethane
7252-83-7

1-bromo-2,2-dimethoxyethane

3-bromomethyl-6-chloro-1,1-dioxo-1,2,3,4-tetrahydro-1λ6-benzo[1,2,4]thiadiazine-7-sulfonic acid amide
7181-60-4

3-bromomethyl-6-chloro-1,1-dioxo-1,2,3,4-tetrahydro-1λ6-benzo[1,2,4]thiadiazine-7-sulfonic acid amide

Conditions
ConditionsYield
With hydrogen bromide In 1,4-dioxane; water at 100 - 120℃; for 0.333333h;100%
chloraminophenamide
121-30-2

chloraminophenamide

5-bromovaleroyl chloride
4509-90-4

5-bromovaleroyl chloride

N-[2,4-bis(aminosulfonyl)-5-chlorophenyl]-5-bromo-pentanamide
907625-19-8

N-[2,4-bis(aminosulfonyl)-5-chlorophenyl]-5-bromo-pentanamide

Conditions
ConditionsYield
In 1,4-dioxane for 2h; Heating / reflux;98%
chloraminophenamide
121-30-2

chloraminophenamide

formic acid
64-18-6

formic acid

chlorothiazide
58-94-6

chlorothiazide

Conditions
ConditionsYield
With sulfuric acid95%
With sulfuric acid
chloraminophenamide
121-30-2

chloraminophenamide

isobutyryl chloride
79-30-1

isobutyryl chloride

N-(5-chloro-2,4-disulfamoyl-phenyl)-isobutyramide
825631-79-6

N-(5-chloro-2,4-disulfamoyl-phenyl)-isobutyramide

Conditions
ConditionsYield
In tetrahydrofuran for 8h; Heating;94%
chloraminophenamide
121-30-2

chloraminophenamide

formaldehyd
50-00-0

formaldehyd

6-chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide
58-93-5

6-chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide

Conditions
ConditionsYield
In water Reflux;92%
In ethanol at 90℃; for 384h;8.36%
With hydrogenchloride; ethyl acetate
chloraminophenamide
121-30-2

chloraminophenamide

2-(2-oxoethyl)benzaldehyde
25705-34-4

2-(2-oxoethyl)benzaldehyde

9-chloro-8-sulfamoyl-4b,5-dihydroisoquino<1,2-c><1,2,4>benzothiadiazine 6,6 dioxide

9-chloro-8-sulfamoyl-4b,5-dihydroisoquino<1,2-c><1,2,4>benzothiadiazine 6,6 dioxide

Conditions
ConditionsYield
With hydrogenchloride In methanol at 20℃;91%
chloraminophenamide
121-30-2

chloraminophenamide

4,4,5,5,6,6,7,7,8,8,9,9,10,10,11,11,11-heptadecafluoroundecanoylchloride
89373-67-1

4,4,5,5,6,6,7,7,8,8,9,9,10,10,11,11,11-heptadecafluoroundecanoylchloride

N-(2,4-disulfamoyl 5-chloro phenyl) 2,2,3,3-tetrahydryl-F-undecanamide

N-(2,4-disulfamoyl 5-chloro phenyl) 2,2,3,3-tetrahydryl-F-undecanamide

Conditions
ConditionsYield
In 1,4-dioxane Heating;90%
chloraminophenamide
121-30-2

chloraminophenamide

quinoline-8-sulfonyl chloride
18704-37-5

quinoline-8-sulfonyl chloride

4-chloro-6-(quinoline-8-sulfonylamino)-benzene-1,3-disulfonic acid diamide

4-chloro-6-(quinoline-8-sulfonylamino)-benzene-1,3-disulfonic acid diamide

Conditions
ConditionsYield
With triethylamine In acetonitrile at 4℃; Alkylation;90%
chloraminophenamide
121-30-2

chloraminophenamide

pentadecafluorooctanoyl chloride
335-64-8

pentadecafluorooctanoyl chloride

2,2,3,3,4,4,5,5,6,6,7,7,8,8,8-Pentadecafluoro-octanoic acid (5-chloro-2,4-disulfamoyl-phenyl)-amide

2,2,3,3,4,4,5,5,6,6,7,7,8,8,8-Pentadecafluoro-octanoic acid (5-chloro-2,4-disulfamoyl-phenyl)-amide

Conditions
ConditionsYield
In 1,4-dioxane Heating;87%
chloraminophenamide
121-30-2

chloraminophenamide

methanol
67-56-1

methanol

4-amino-1,3-benzenedisulfonamide
40642-90-8

4-amino-1,3-benzenedisulfonamide

Conditions
ConditionsYield
In water Product distribution; Mechanism; Irradiation; multistep reaction, photholytic decomposition; also in pure MeOH;85%
chloraminophenamide
121-30-2

chloraminophenamide

2-benzoylbenzaldehyde
16780-82-8

2-benzoylbenzaldehyde

2-Chloro-3-sulfamoyl-11-phenyl-11H-isoindolo<1,2-c><1,2,4>benzothiadiazine 5,5-dioxide

2-Chloro-3-sulfamoyl-11-phenyl-11H-isoindolo<1,2-c><1,2,4>benzothiadiazine 5,5-dioxide

Conditions
ConditionsYield
With hydrogenchloride In methanol at 20℃; for 24h;85%
chloraminophenamide
121-30-2

chloraminophenamide

undecafluorohexanoyl chloride
335-53-5

undecafluorohexanoyl chloride

2,2,3,3,4,4,5,5,6,6,6-Undecafluoro-hexanoic acid (5-chloro-2,4-disulfamoyl-phenyl)-amide

2,2,3,3,4,4,5,5,6,6,6-Undecafluoro-hexanoic acid (5-chloro-2,4-disulfamoyl-phenyl)-amide

Conditions
ConditionsYield
In 1,4-dioxane Heating;81%
chloraminophenamide
121-30-2

chloraminophenamide

4,5-dimethoxy-phthalaldehyde
43073-12-7

4,5-dimethoxy-phthalaldehyde

2-Chloro-3-sulfamoyl-8,9-dimethoxy-11H-isoindolo<1,2-c><1,2,4>benzothiadiazine 5,5-dioxide

2-Chloro-3-sulfamoyl-8,9-dimethoxy-11H-isoindolo<1,2-c><1,2,4>benzothiadiazine 5,5-dioxide

Conditions
ConditionsYield
With hydrogenchloride In methanol at 20℃; for 24h;81%
chloraminophenamide
121-30-2

chloraminophenamide

isovaleraldehyde
590-86-3

isovaleraldehyde

(R)-thiabutazide
96783-07-2

(R)-thiabutazide

Conditions
ConditionsYield
With C64H73O4P In dichloromethane at 20℃; for 168h; Inert atmosphere; Molecular sieve; optical yield given as %ee; enantioselective reaction;81%
chloraminophenamide
121-30-2

chloraminophenamide

2,3-naphthalenedicarboxaldehyde
7149-49-7

2,3-naphthalenedicarboxaldehyde

2-Chloro-3-sulfamoyl-13H-benzo<5,6>isoindolo<1,2-c><1,2,4>benzothiadiazine 5,5-dioxide

2-Chloro-3-sulfamoyl-13H-benzo<5,6>isoindolo<1,2-c><1,2,4>benzothiadiazine 5,5-dioxide

Conditions
ConditionsYield
With hydrogenchloride In methanol at 20℃; for 24h;80%
chloraminophenamide
121-30-2

chloraminophenamide

isovaleraldehyde
590-86-3

isovaleraldehyde

Conditions
ConditionsYield
With 2,6-bis[(3aR,8aS)-3a,8a-dihydro-8H-indeno[1,2-d]oxazolin-2-yl]pyridine; scandium tris(trifluoromethanesulfonate) In dichloromethane at -40℃; for 24h; Molecular sieve; Schlenk technique;79%
With hydrogenchloride In diethylene glycol dimethyl ether Heating;
With hydrogenchloride In ethanol Heating;
With hydrogenchloride Heating;
chloraminophenamide
121-30-2

chloraminophenamide

4-piperidone hydrochloride
41979-39-9

4-piperidone hydrochloride

spiro[2H-1,2,4-benzothiadiazine-3(4H),4'-piperidine]-7-sulfonamide-6-chloro-1,1-dioxide monohydrochloride
6451-58-7

spiro[2H-1,2,4-benzothiadiazine-3(4H),4'-piperidine]-7-sulfonamide-6-chloro-1,1-dioxide monohydrochloride

Conditions
ConditionsYield
toluene-4-sulfonic acid In N,N-dimethyl acetamide; toluene at 180 - 200℃; for 3 - 4h;76.4%
chloraminophenamide
121-30-2

chloraminophenamide

5-bromo-2-isocyanatobenzofuran

5-bromo-2-isocyanatobenzofuran

3-(5-bromo-1-benzofuran-2-yl)-1-(5-chloro-2,4-disulfamoylphenyl)urea

3-(5-bromo-1-benzofuran-2-yl)-1-(5-chloro-2,4-disulfamoylphenyl)urea

Conditions
ConditionsYield
In toluene for 6h; Reflux;75%
chloraminophenamide
121-30-2

chloraminophenamide

2-cyclopentylacetaldehyde
5623-81-4

2-cyclopentylacetaldehyde

(R)-cyclopenthiazide
1087345-33-2

(R)-cyclopenthiazide

Conditions
ConditionsYield
With C64H73O4P In dichloromethane at 20℃; for 168h; Inert atmosphere; Molecular sieve; optical yield given as %ee; enantioselective reaction;74%
chloraminophenamide
121-30-2

chloraminophenamide

ethanol
64-17-5

ethanol

(+/-)-6-chloro-3-methyl-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide
890-67-5

(+/-)-6-chloro-3-methyl-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide

Conditions
ConditionsYield
With tert.-butylhydroperoxide at 110℃; for 12h;73%
chloraminophenamide
121-30-2

chloraminophenamide

isovaleraldehyde
590-86-3

isovaleraldehyde

C11H16ClN3O4S2

C11H16ClN3O4S2

Conditions
ConditionsYield
With C60H96O10 In toluene at 20℃; for 70h; Inert atmosphere; Schlenk technique; Molecular sieve;72%
chloraminophenamide
121-30-2

chloraminophenamide

2,6-Pyridinedicarbonyl dichloride
3739-94-4

2,6-Pyridinedicarbonyl dichloride

N2,N6-bis(5-chloro-2,4-disulfamoylphenyl)pyridine-2,6-dicarboxamide

N2,N6-bis(5-chloro-2,4-disulfamoylphenyl)pyridine-2,6-dicarboxamide

Conditions
ConditionsYield
In dichloromethane; acetone at 20℃; for 12h;72%
chloraminophenamide
121-30-2

chloraminophenamide

heptafluorobutyryl chloride
375-16-6

heptafluorobutyryl chloride

N-(5-Chloro-2,4-disulfamoyl-phenyl)-2,2,3,3,4,4,4-heptafluoro-butyramide

N-(5-Chloro-2,4-disulfamoyl-phenyl)-2,2,3,3,4,4,4-heptafluoro-butyramide

Conditions
ConditionsYield
In 1,4-dioxane Heating;70%
chloraminophenamide
121-30-2

chloraminophenamide

[14C]formaldehyde
3046-49-9

[14C]formaldehyde

[3-14C]hydrochlorothiazide
1441369-99-8

[3-14C]hydrochlorothiazide

Conditions
ConditionsYield
In tetrahydrofuran at -78 - 140℃; Microwave irradiation;69%
chloraminophenamide
121-30-2

chloraminophenamide

methanol
67-56-1

methanol

6-chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide
58-93-5

6-chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide

Conditions
ConditionsYield
With tert.-butylhydroperoxide at 110℃; for 12h;63%
chloraminophenamide
121-30-2

chloraminophenamide

2-bromo-4-chlorobenzene-1,5-disulfonamide
74724-36-0

2-bromo-4-chlorobenzene-1,5-disulfonamide

Conditions
ConditionsYield
Stage #1: chloraminophenamide With sulfuric acid; sodium nitrite In acetonitrile at 0 - 40℃;
Stage #2: With copper(ll) bromide In water; acetonitrile at 0 - 80℃;
62%
chloraminophenamide
121-30-2

chloraminophenamide

C10H7NO2

C10H7NO2

1-(5-chloro-2,4-disulfamoylphenyl)-3-(3-methyl-1-benzofuran-2-yl)urea

1-(5-chloro-2,4-disulfamoylphenyl)-3-(3-methyl-1-benzofuran-2-yl)urea

Conditions
ConditionsYield
In toluene for 6h; Reflux;61%
chloraminophenamide
121-30-2

chloraminophenamide

C15H15N3OS

C15H15N3OS

4-chloro-6-((3-(3-methylbenzo[4,5]imidazo[2,1-b]thiazol-2-yl)-3-oxoprop-1-en-1-yl)amino)benzene-1,3-disulfonamide

4-chloro-6-((3-(3-methylbenzo[4,5]imidazo[2,1-b]thiazol-2-yl)-3-oxoprop-1-en-1-yl)amino)benzene-1,3-disulfonamide

Conditions
ConditionsYield
With acetic acid for 5h; Reflux;60%
chloraminophenamide
121-30-2

chloraminophenamide

o-phthalic dicarboxaldehyde
643-79-8

o-phthalic dicarboxaldehyde

2-Chloro-3-sulfamoyl-11H-isoindolo<1,2-c><1,2,4>benzothiadiazine 5,5-dioxide

2-Chloro-3-sulfamoyl-11H-isoindolo<1,2-c><1,2,4>benzothiadiazine 5,5-dioxide

Conditions
ConditionsYield
With hydrogenchloride In methanol at 20℃; for 24h;59%

121-30-2Related news

Photocatalytic degradation of 4-Amino-6-chlorobenzene-1,3-disulfonamide (cas 121-30-2) stable hydrolysis product of hydrochlorothiazide: Detection of intermediates and their toxicity☆09/04/2019

In this work we have investigated in details the process of degradation of the 4-amino-6-chlorobenzene-1,3-disulfonamide (ABSA), stable hydrolysis product of frequently used pharmaceutical hydrochlorothiazide (HCTZ), as one of the most ubiquitous contaminants in the sewage water. The study encom...detailed

121-30-2Relevant articles and documents

Adsorption of benzothiadiazines by carbon black from aqueous solution, and related phenomena

Ueda,Nambu,Nagai

, p. 3426 - 3430 (1980)

-

Stability-indicating assay for hydrochlorothiazide

Daniels,Vanderwielen

, p. 211 - 215 (1981)

A stability-indicating method for determining hydrochlorothiazide in tablet formulations and in the bulk form is described. Hydrochlorothiazide is dissolved or extracted using methanol. An aliquot of the solution, containing sulfadiazine as an internal standard, is chromatographed on a 10-μm C18 column with an aqueous mobile phase containing 5% methanol as the modifier. The pH is adjusted to about 4.5 with acetic acid. The method gave accurate results for nine lots (four different suppliers) of tablets and two bulk drug lots (two different suppliers). The assay has a relative standard deviation of about 1%. The method can also be used as a test for impurities in hydrochlorothiazide. The data in this study indicate that the test should give accurate results for impurities between 0.1 and 5%.

Accelerated Forced Degradation of Pharmaceuticals in Levitated Microdroplet Reactors

Li, Yangjie,Liu, Yong,Gao, Hong,Helmy, Roy,Wuelfing, W. Peter,Welch, Christopher J.,Cooks, R. Graham

, p. 7349 - 7353 (2018)

Forced degradation is a method of studying the stability of pharmaceuticals in order to design stable formulations and predict drug product shelf life. Traditional methods of reaction and analysis usually take multiple days, and include LC-UV and LC-MS product analysis. In this study, the reaction/analysis sequence was accelerated to be completed within minutes using Leidenfrost droplets as reactors (acceleration factor: 23–188) and nanoelectrospray ionization MS analysis. The Leidenfrost droplets underwent the same reactions as seen in traditional bulk solution experiments for three chemical degradations studied. This combined method of accelerated reaction and analysis has the potential to be extended to forced degradation of other pharmaceuticals and to drug formulations. Control of reaction rate and yield is achieved by manipulating droplet size, levitation time and whether or not make-up solvent is added. Evidence is provided that interfacial effects contribute to rate acceleration.

Weinstok,R.,Kratzl,K.

, p. 1586 - 1591 (1965)

Epimerization and racemization of some chiral drugs in the presence of human serum albumin

Aso,Yoshioka,Takeda

, p. 180 - 184 (2007/10/02)

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