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863031-21-4

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  • High Quality 99% 1H-Benzimidazole-7-carboxylic acid, 1-[[2'-(2,5-dihydro-5-oxo-1,2,4-oxadiazol-3-yl)[1,1'-biphenyl]-4-yl]methyl]-2-ethoxy-, (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl ester 863031-21-4 ISO

    Cas No: 863031-21-4

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  • 1H-Benzimidazole-7-carboxylic acid, 1-[[2'-(2,5-dihydro-5-oxo-1,2,4-oxadiazol-3-yl)[1,1'-biphenyl]-4-yl]methyl]-2-ethoxy-, (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl ester

    Cas No: 863031-21-4

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863031-21-4 Usage

Description

Different sources of media describe the Description of 863031-21-4 differently. You can refer to the following data:
1. Azilsartan medoxomil (Edarbi), an angiotensin II receptor antagonist, was approved by the U.S. FDA in February 2011 for the treatment of hypertension in adults. The discovery of azilsartan was the result of a medicinal chemistry effort to identify an ARB with a different carboxylic acid isostere than the ones found in the marketed ARBs. Several of the marketed ARBs use a tetrazole group as a carboxylic acid isostere. The medicinal chemistry approach that led to azilsartan involved the replacement of this commonly used tetrazole with a 5-oxo-1,2,4-oxadiazole group. Azilsartan can be synthesized by Suzuki coupling of p-tolyl boronic acid to 2-bromobenzonitrile, followed by bromination of the methyl group. The bromide is displaced to introduce a protected 2-ethoxy-1H-benzo[d] imidazole-7-carboxylate. The cyano group is converted to a hydroxylamidine, followed by reaction with an alkyl-chloroformate and intramolecular cyclization to form the 5-oxo-1,2,4-oxadiazole ring. The acid is then deprotected and converted to a prodrug. The parent, azilsartan has been extensively characterized in vitro and compared with other marketed AT1 antagonists olmesartan, valsartan, telmisartan, irbesartan, and candesartan. Azilsartan was found to be a potent (IC50=2.6 nM), selective, inverse agonist of the AT1 receptor. From washout experiments, azilsartan was found have slow dissociation from the receptor and thus is characterized as an insurmountable antagonist.
2. Azilsartan medoxomil is a prodrug form of azilsartan , a potent and selective angiotensin II receptor 1 (AT1) antagonist. Azilsartan medoxomil (0.1-10 mg/kg) reduces blood pressure and decreases plasminogen activator inhibitor 1 (PAI-1) levels in the plasma, left ventricle, and aortic wall in mice in a dose-dependent manner. It also inhibits the pressor response induced by angiotensin II in normotensive rats (ID50 = 0.12 mg/kg) and reduces blood pressure and improves glucose infusion, a marker of insulin sensitivity, in spontaneously hypertensive rats. Azilsartan medoxomil also has more potent antiproteinuric effects in Wistar fatty rats than olmesartan medoxomil . Formulations containing azilsartan medoxomil have been used in the treatment of hypertension.

Originator

Takeda (United States)

Uses

Azilsartan medoxomil is a long-acting angiotensin II receptor blocker (ARB) that is used to lower hypertension. When Azilsartan medoxomil enters the gastrointestinal tract, it is rapidly converted to its active form, Azilsartan (A926900).

Definition

ChEBI: A carboxylic ester obtained by formal condensation of the carboxy group of azilsartan with the hydroxy group of 4-(hydroxymethyl)-5-methyl-1,3-dioxol-2-one. A prodrug for azilsartan, it is used for treatment of hypertension.

Brand name

Edarbi

Check Digit Verification of cas no

The CAS Registry Mumber 863031-21-4 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,6,3,0,3 and 1 respectively; the second part has 2 digits, 2 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 863031-21:
(8*8)+(7*6)+(6*3)+(5*0)+(4*3)+(3*1)+(2*2)+(1*1)=144
144 % 10 = 4
So 863031-21-4 is a valid CAS Registry Number.
InChI:InChI:1S/C30H24N4O8/c1-3-38-28-31-23-10-6-9-22(27(35)39-16-24-17(2)40-30(37)41-24)25(23)34(28)15-18-11-13-19(14-12-18)20-7-4-5-8-21(20)26-32-29(36)42-33-26/h4-14H,3,15-16H2,1-2H3,(H,32,33,36)

863031-21-4SDS

SAFETY DATA SHEETS

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

Version: 1.0

Creation Date: Aug 14, 2017

Revision Date: Aug 14, 2017

1.Identification

1.1 GHS Product identifier

Product name azilsartan medoxomil

1.2 Other means of identification

Product number -
Other names (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl ester of 1-[[2'-(2,5-dihydro-5-oxo-1,2,4-oxadiazol-3-yl)[1,1'-biphenyl]-4-yl]methyl]-2-ethoxy-1H-benzimidazole-7-carboxylic acid

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:863031-21-4 SDS

863031-21-4Synthetic route

Carbonyldiimidazole
64269-79-0

Carbonyldiimidazole

(5-methyl-2-oxo-2H-1,3-dioxol-4yl)methyl 2-ethoxy-1-[(4-(2-[N-hydroxy-carbamimidoyl]phenyl)phenyl)-methyl]-1H-1,3-benzodiazole-7-carboxylate
1449029-77-9

(5-methyl-2-oxo-2H-1,3-dioxol-4yl)methyl 2-ethoxy-1-[(4-(2-[N-hydroxy-carbamimidoyl]phenyl)phenyl)-methyl]-1H-1,3-benzodiazole-7-carboxylate

Azilsartan medoxomil
863031-21-4

Azilsartan medoxomil

Conditions
ConditionsYield
In dimethyl sulfoxide at 50℃; for 2h;98.2%
4-hydroxymethyl-5-methyl-[1,3]dioxol-2-one
91526-18-0

4-hydroxymethyl-5-methyl-[1,3]dioxol-2-one

azilsartan
147403-03-0

azilsartan

Azilsartan medoxomil
863031-21-4

Azilsartan medoxomil

Conditions
ConditionsYield
Stage #1: 4-hydroxymethyl-5-methyl-[1,3]dioxol-2-one; azilsartan With dmap; potassium carbonate; p-toluenesulfonyl chloride In N,N-dimethyl acetamide at 10℃; for 3h;
Stage #2: In N,N-dimethyl acetamide pH=5;
Stage #3: In water; acetone at 35℃; for 2h;
95%
Stage #1: 4-hydroxymethyl-5-methyl-[1,3]dioxol-2-one; azilsartan With dmap; p-toluoylsulfonylchloride; potassium carbonate In ISOPROPYLAMIDE at -15 - 25℃;
Stage #2: With hydrogenchloride In ISOPROPYLAMIDE; water for 0.5h; pH=4 - 5;
81%
With dmap; potassium carbonate; p-toluenesulfonyl chloride In N,N-dimethyl acetamide at 8 - 10℃; for 3h;80.1%
(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 2-ethoxy-1-{[2'-(N'-{[(4-nitrophenoxy)carbonyl]oxy}carbamimidoyl)biphenyl-4-yl]methyl}-1H-benzimidazole-7-carboxylate
1449029-80-4

(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 2-ethoxy-1-{[2'-(N'-{[(4-nitrophenoxy)carbonyl]oxy}carbamimidoyl)biphenyl-4-yl]methyl}-1H-benzimidazole-7-carboxylate

Azilsartan medoxomil
863031-21-4

Azilsartan medoxomil

Conditions
ConditionsYield
at 20 - 60℃; for 12h; Solvent; Temperature;87%
With 2-methylpropyl acetate at 20 - 60℃; for 12h; Reagent/catalyst; Temperature;87%
(5-methyl-2-oxo-2H-1,3-dioxol-4yl)methyl 2-ethoxy-1-[(4-(2-[N-hydroxy-carbamimidoyl]phenyl)phenyl)-methyl]-1H-1,3-benzodiazole-7-carboxylate
1449029-77-9

(5-methyl-2-oxo-2H-1,3-dioxol-4yl)methyl 2-ethoxy-1-[(4-(2-[N-hydroxy-carbamimidoyl]phenyl)phenyl)-methyl]-1H-1,3-benzodiazole-7-carboxylate

Azilsartan medoxomil
863031-21-4

Azilsartan medoxomil

Conditions
ConditionsYield
With di(succinimido) carbonate In ethyl acetate at 25 - 45℃; for 16h; Solvent; Reagent/catalyst; Temperature; Large scale;82%
Multi-step reaction with 2 steps
1: triethylamine / dichloromethane / 1.5 h / 0 - 30 °C
2: 10 h / 20 - 115 °C
View Scheme
Multi-step reaction with 2 steps
1: sodium hydrogencarbonate / dichloromethane; water / 1 h / 20 - 30 °C
2: 12 h / 20 - 60 °C
View Scheme
Multi-step reaction with 2 steps
1: sodium hydrogencarbonate / water; dichloromethane / 1 h / 20 - 30 °C
2: 2-methylpropyl acetate / 12 h / 20 - 60 °C
View Scheme
(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl ester of 1-[[2'-(2,5-dihydro-5-oxo-1,2,4-oxadiazol-3-yl)[1,1'-biphenyl]-4-yl]methyl]-2-ethoxy-1H-benzimidazole-7-carboxylic acid dimethylacetamide
1417575-99-5

(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl ester of 1-[[2'-(2,5-dihydro-5-oxo-1,2,4-oxadiazol-3-yl)[1,1'-biphenyl]-4-yl]methyl]-2-ethoxy-1H-benzimidazole-7-carboxylic acid dimethylacetamide

Azilsartan medoxomil
863031-21-4

Azilsartan medoxomil

Conditions
ConditionsYield
In water; acetone Reflux;78%
(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl-2-ethoxy-1H-benzo[d]imidazol-7-carboxylate

(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl-2-ethoxy-1H-benzo[d]imidazol-7-carboxylate

3-(4'-(bromomethyl)-[1,1'-biphenyl]-2-yl)-1,2,4-oxadiazol-5(4H)-one

3-(4'-(bromomethyl)-[1,1'-biphenyl]-2-yl)-1,2,4-oxadiazol-5(4H)-one

Azilsartan medoxomil
863031-21-4

Azilsartan medoxomil

Conditions
ConditionsYield
Stage #1: (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl-2-ethoxy-1H-benzo[d]imidazol-7-carboxylate In ethanol at 20℃; for 0.166667h;
Stage #2: 3-(4'-(bromomethyl)-[1,1'-biphenyl]-2-yl)-1,2,4-oxadiazol-5(4H)-one With tetrabutylammomium bromide; potassium carbonate In ethanol at 40 - 50℃; for 10h; Reagent/catalyst; Temperature;
77.9%
With potassium carbonate; potassium iodide In dichloromethane Reflux;72%
2-ethoxy-1-((2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylic acid dicyclohexylamine salt

2-ethoxy-1-((2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylic acid dicyclohexylamine salt

Azilsartan medoxomil
863031-21-4

Azilsartan medoxomil

Conditions
ConditionsYield
Stage #1: 2-ethoxy-1-((2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylic acid dicyclohexylamine salt at 23 - 28℃; for 0.5h;
Stage #2: With 4-chloromethyl-5-methyl-1,3-dioxol-2-one; potassium iodide at 50℃; for 3h;
76%
1-[{2’-(2,5-dihydro-5-oxo-1,2,4-oxodiazol-3-yl)(1,1’-biphenyl)-4-yl}methyl]-2-ethoxy-1H-benzimidazole-7-carboxylic acid (5-methyl-2-oxo-1,3-dioxol-4-yl) methyl ester potassium salt

1-[{2’-(2,5-dihydro-5-oxo-1,2,4-oxodiazol-3-yl)(1,1’-biphenyl)-4-yl}methyl]-2-ethoxy-1H-benzimidazole-7-carboxylic acid (5-methyl-2-oxo-1,3-dioxol-4-yl) methyl ester potassium salt

Azilsartan medoxomil
863031-21-4

Azilsartan medoxomil

Conditions
ConditionsYield
In water at 50 - 55℃; for 2h;55%
disodium 2-ethoxy-1-{[2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl}-1H-benzimidazole-7-carboxylate

disodium 2-ethoxy-1-{[2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl}-1H-benzimidazole-7-carboxylate

4-chloromethyl-5-methyl-1,3-dioxol-2-one
80841-78-7

4-chloromethyl-5-methyl-1,3-dioxol-2-one

Azilsartan medoxomil
863031-21-4

Azilsartan medoxomil

Conditions
ConditionsYield
Stage #1: disodium 2-ethoxy-1-{[2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl}-1H-benzimidazole-7-carboxylate; 4-chloromethyl-5-methyl-1,3-dioxol-2-one In N,N-dimethyl-formamide at 20℃; for 12h;
Stage #2: With hydrogenchloride In chloroform; water
14%
C32H21Cl3N4O6

C32H21Cl3N4O6

4-hydroxymethyl-5-methyl-[1,3]dioxol-2-one
91526-18-0

4-hydroxymethyl-5-methyl-[1,3]dioxol-2-one

Azilsartan medoxomil
863031-21-4

Azilsartan medoxomil

Conditions
ConditionsYield
With dmap In dichloromethane at 20℃; for 4h;
4-chloromethyl-5-methyl-1,3-dioxol-2-one
80841-78-7

4-chloromethyl-5-methyl-1,3-dioxol-2-one

Azilsartan medoxomil
863031-21-4

Azilsartan medoxomil

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1.1: triethylamine; formic acid / acetonitrile / 10 - 65 °C
1.2: Reflux
2.1: dmap; potassium carbonate; p-toluoylsulfonylchloride / ISOPROPYLAMIDE / -15 - 25 °C
2.2: 0.5 h / pH 4 - 5
View Scheme
methyl 1-[(2'-cyanobiphenyl-4-yl)methyl]-2-ethoxy-benzimidazole-7-carboxylate
139481-44-0

methyl 1-[(2'-cyanobiphenyl-4-yl)methyl]-2-ethoxy-benzimidazole-7-carboxylate

Azilsartan medoxomil
863031-21-4

Azilsartan medoxomil

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1.1: hydroxylamine hydrochloride; sodium hydrogencarbonate / dimethyl sulfoxide / 18 h / 25 - 90 °C
2.1: 1,8-diazabicyclo[5.4.0]undec-7-ene / tetrahydrofuran / 20 - 25 °C
3.1: sodium hydroxide; water / 0.5 h / 50 - 55 °C
3.2: 0.5 h / 20 - 25 °C / pH 2 - 3
4.1: dmap; potassium carbonate; p-toluoylsulfonylchloride / ISOPROPYLAMIDE / -15 - 25 °C
4.2: 0.5 h / pH 4 - 5
View Scheme
Multi-step reaction with 4 steps
1: hydroxylamine hydrochloride / dimethyl sulfoxide; water / 18 h / 90 °C
2: potassium carbonate / dimethyl sulfoxide / 4 h / 20 °C
3: sodium hydroxide; water / 3 h / 50 °C
4: potassium carbonate; p-toluenesulfonyl chloride; dmap / N,N-dimethyl acetamide / 3 h / 30 °C
View Scheme
Multi-step reaction with 4 steps
1: hydroxylamine hydrochloride / dimethyl sulfoxide; water / 18 h / 90 °C
2: 1,8-diazabicyclo[5.4.0]undec-7-ene / dimethyl sulfoxide / 4 h / 20 °C
3: sodium hydroxide; water / 3 h / 50 °C
4: potassium carbonate; p-toluenesulfonyl chloride; dmap / N,N-dimethyl acetamide / 3 h / 30 °C
View Scheme
methyl 2-ethoxy-1-((2′-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl)methyl)-1H-benzo[d]-imidazole-7-carboxylate
147403-52-9

methyl 2-ethoxy-1-((2′-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl)methyl)-1H-benzo[d]-imidazole-7-carboxylate

Azilsartan medoxomil
863031-21-4

Azilsartan medoxomil

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1.1: sodium hydroxide; water / 0.5 h / 50 - 55 °C
1.2: 0.5 h / 20 - 25 °C / pH 2 - 3
2.1: dmap; potassium carbonate; p-toluoylsulfonylchloride / ISOPROPYLAMIDE / -15 - 25 °C
2.2: 0.5 h / pH 4 - 5
View Scheme
Multi-step reaction with 2 steps
1: sodium hydroxide; water / 3 h / 50 °C
2: potassium carbonate; p-toluenesulfonyl chloride; dmap / N,N-dimethyl acetamide / 3 h / 30 °C
View Scheme
methyl 2-ethoxy-1-((2′-(N′-hydroxycarbamimidoyl)-biphenyl-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate
147403-65-4

methyl 2-ethoxy-1-((2′-(N′-hydroxycarbamimidoyl)-biphenyl-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate

Azilsartan medoxomil
863031-21-4

Azilsartan medoxomil

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1.1: 1,8-diazabicyclo[5.4.0]undec-7-ene / tetrahydrofuran / 20 - 25 °C
2.1: sodium hydroxide; water / 0.5 h / 50 - 55 °C
2.2: 0.5 h / 20 - 25 °C / pH 2 - 3
3.1: dmap; potassium carbonate; p-toluoylsulfonylchloride / ISOPROPYLAMIDE / -15 - 25 °C
3.2: 0.5 h / pH 4 - 5
View Scheme
Multi-step reaction with 3 steps
1: 1,8-diazabicyclo[5.4.0]undec-7-ene / dimethyl sulfoxide / 4 h / 20 °C
2: sodium hydroxide; water / 3 h / 50 °C
3: potassium carbonate; p-toluenesulfonyl chloride; dmap / N,N-dimethyl acetamide / 3 h / 30 °C
View Scheme
Multi-step reaction with 3 steps
1: potassium carbonate / dimethyl sulfoxide / 4 h / 20 °C
2: sodium hydroxide; water / 3 h / 50 °C
3: potassium carbonate; p-toluenesulfonyl chloride; dmap / N,N-dimethyl acetamide / 3 h / 30 °C
View Scheme
ethyl 1-[(2'-cyano-[1,1']-biphenyl-4-yl)methyl]-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate
139481-41-7

ethyl 1-[(2'-cyano-[1,1']-biphenyl-4-yl)methyl]-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate

Azilsartan medoxomil
863031-21-4

Azilsartan medoxomil

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1: hydroxylamine hydrochloride / dimethyl sulfoxide; water / 15 h / 90 °C
2: dimethyl sulfoxide; methanol / 2 h / 20 - 25 °C
3: sodium hydroxide; water / 3 h / 50 °C
4: potassium carbonate; p-toluenesulfonyl chloride; dmap / N,N-dimethyl acetamide / 3 h / 30 °C
View Scheme
ethyl 2-ethoxy-1-((2′-(N′-hydroxycarbamimidoyl)biphenyl-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate
1397836-41-7

ethyl 2-ethoxy-1-((2′-(N′-hydroxycarbamimidoyl)biphenyl-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate

Azilsartan medoxomil
863031-21-4

Azilsartan medoxomil

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: dimethyl sulfoxide; methanol / 2 h / 20 - 25 °C
2: sodium hydroxide; water / 3 h / 50 °C
3: potassium carbonate; p-toluenesulfonyl chloride; dmap / N,N-dimethyl acetamide / 3 h / 30 °C
View Scheme
4-hydroxymethyl-5-methyl-[1,3]dioxol-2-one
91526-18-0

4-hydroxymethyl-5-methyl-[1,3]dioxol-2-one

4-Nitrobenzenesulfonyl chloride
98-74-8

4-Nitrobenzenesulfonyl chloride

azilsartan
147403-03-0

azilsartan

Azilsartan medoxomil
863031-21-4

Azilsartan medoxomil

Conditions
ConditionsYield
Stage #1: azilsartan With dmap; triethylamine In dichloromethane at 0 - 5℃; for 0.0833333h;
Stage #2: 4-Nitrobenzenesulfonyl chloride In dichloromethane at 0 - 30℃; for 1h;
Stage #3: 4-hydroxymethyl-5-methyl-[1,3]dioxol-2-one In N,N-dimethyl-formamide at 20 - 40℃; for 1h;
6.5 g
(2-ethoxy-1-{[2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl}-1H-benzimidazol-7-yl)-carboxyl-4-nitrophenyl sulfonate
1427268-39-0

(2-ethoxy-1-{[2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl}-1H-benzimidazol-7-yl)-carboxyl-4-nitrophenyl sulfonate

4-hydroxymethyl-5-methyl-[1,3]dioxol-2-one
91526-18-0

4-hydroxymethyl-5-methyl-[1,3]dioxol-2-one

Azilsartan medoxomil
863031-21-4

Azilsartan medoxomil

Conditions
ConditionsYield
Stage #1: (2-ethoxy-1-{[2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl}-1H-benzimidazol-7-yl)-carboxyl-4-nitrophenyl sulfonate In dichloromethane at 20 - 30℃; for 0.0833333h;
Stage #2: 4-hydroxymethyl-5-methyl-[1,3]dioxol-2-one With dmap In dichloromethane at 20 - 45℃; for 2h;
5.1 g

863031-21-4Relevant articles and documents

Polymorphs and solvatomorphs of azilsartan medoxomil: Elucidation of solvent-induced construction and conformational diversity

Zhang, Xian-Rui,He, Sai-Fei,Zhang, Shuo,Li, Jing,Li, Shan,Liu, Jin-Song,Zhang, Lei

, p. 103 - 113 (2017)

Two polymorphs (AM-A and AM-B) of azilsartan medoxomil (AM) and four AM solvatomorphs with toluene (AM-TOL), 1,4-dioxane (AM-DIO), chloroform (AM-TCM) and N,N-dimethylacetamide (AM-DMA) have been prepared by the hydrolysis of azilsartan medoxomil potassium in aqueous-organic solutions. In the crystal structures of two polymorphs and three solvatomorphs (AM-TOL, AM-DIO and AM-TCM), two asymmetric AM molecules form the dimeric cycle-like structures via intermolecular N[sbnd]H?N hydrogen bonds in R22 (26) ring, while AM-DMA shows intramolecular N[sbnd]H?O hydrogen bond between AM and DMA molecules. The hydrogen bonds (C[sbnd]H?O or C[sbnd]H?N) and π···π (or C[sbnd]H···π) interactions are helpful to stabilize the conformational diversity of AM. The solvent-induced experiment shows that solvent molecules have great influence on the solvatomorph formation and DIO can form the most steady solvatomorph than other solvents. The thermal study demonstrates that toluene molecules in three solvatomorphs (AM-TOL, AM-DIO and AM-TCM) are the most difficult to remove from the cage. Our results illustrate that the solvent plays significant role in tuning the size of the cage and producing the conformational diversity of AM molecules.

Preparation method of azilsartan kamedoxomil hydrate

-

Paragraph 0061; 0064, (2018/09/08)

The invention provides a preparation method of azilsartan kamedoxomil hydrate. The preparation method at least comprises the following steps: (1) performing the chlorination; (2) performing the esterification; (3) forming azilsartan kamedoxomil; and (4) forming the azilsartan kamedoxomil hydrate. The preparation method has the characteristics of simple operation, high yield, high purity and good stability, and is suitable for industrialized production.

A method for preparing arab League Qi Shatan ester (by machine translation)

-

Paragraph 0018 - 0021; 0046 - 0049, (2016/10/08)

The invention relates to a method of synthesizing arab League Qi Shatan ester, the method to the 4 [...] -bromo methyl-2-cyano biphenyl as the raw material and then by the hydroxylamine compound II is prepared by cyclization; to 2-ethoxylbenzimidazole-7-carboxylic acid as raw materials to carry out the esterification reaction to make compound V, then utilize the compound prepared with compound II arab League Qi Shatan ester V reaction. The method of the present invention the synthetic route is short, the operation is simple, high yield, at the same time reduces the raw material 4 the [...] -bromomethyl-2-cyanobiphenyl consumption, the cost is reduced. (by machine translation)

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