Candesartan cilexetil supplier

Name
Candesartan cilexetil
EINECS 627-030-2
CAS No. 145040-37-5
Article Data41
CAS DataBase
Density 1.37 g/cm³
Solubility
Melting Point 168-170?C
Formula C₃₃H₃₄N₆O₆
Boiling Point 843.3 ºC at 760 mmHg
Molecular Weight 610.67
Flash Point 463.8 ºC
Transport Information
Appearance White crystalline powder
Safety 26-36
Risk Codes 20/21/22-36/37/38
Molecular Structure
Hazard Symbols Xn
Synonyms 1H-Benzimidazolium, 7-carboxy-1-(2-((cyclohexylcarbonyl)oxy)ethyl)-2-ethoxy-1-(2-(1H-tetrazol-5-yl)(1,1-biphenyl)-4-yl)-, hydroxide, inner salt, (+-)-;TCV-116;Atacand;Atacand (TN);1-cyclohexyloxycarbonyloxyethyl 2-ethoxy-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]benzoimidazole-4-carboxylate;TCV 116;Candesartancilexetil;
PSA 143.34000
LogP 6.31910

Synthetic route

: 170791-09-0
cilexetil trityl candesartan

: 145040-37-5
candesartan cilexetil

Conditions

Conditions	Yield
With hydrogenchloride In methanol; dichloromethane at -14 - -12℃; Temperature; Flow reactor; Large scale;	98%
With iron(III) chloride In methanol; dichloromethane at 23℃; for 48h; Time; Reagent/catalyst;	96%
With methanol; zinc(II) chloride In butanone at 20 - 40℃; for 2.5h; Product distribution / selectivity;	95.23%

: 78-09-1
orthocarbonic acid tetraethyl ester

: 1236156-65-2
2-(((2'-(1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)amino)-3-aminobenzoic acid-1-(((cyclohexyloxy)carbonyl)oxy)ethyl ester

: 145040-37-5
candesartan cilexetil

Conditions

Conditions	Yield
With acetic acid In ethyl acetate at 30℃; Temperature;	93.9%
With acetic acid In toluene at 60℃; for 2h;	81%

: 78-09-1
orthocarbonic acid tetraethyl ester

: C30H32N6O5*C2H2O4

: 145040-37-5
candesartan cilexetil

Conditions

Conditions	Yield
Stage #1: C30H32N6O5*C2H2O4 With potassium carbonate In ethyl acetate at 10 - 15℃; pH=6 - 7; Stage #2: orthocarbonic acid tetraethyl ester In acetic acid at 0 - 25℃; for 15h;	92.3%

: 1307853-85-5
1-{[(cyclohexyloxy)carbonyl]oxy}ethyl 1-({4-[2-(1-benzyl-1H-1,2,3,4-tetrazol-5-yl)phenyl]phenyl}methyl)-2-ethoxy-1H-1,3-benzodiazole-7-carboxylate

: 145040-37-5
candesartan cilexetil

Conditions

Conditions	Yield
With 5% palladium on barium sulphate; ammonium formate In water; isopropyl alcohol at 25℃; for 14h; Temperature; Time;	92.1%
With 5% palladium on barium sulphate; ammonium formate In water; isopropyl alcohol at 25℃; for 14h;	80%
With ammonium formate; palladium over charcoal In water; isopropyl alcohol at 55 - 60℃; for 12 - 15h;
With rosenmund catalyst; ammonium formate In water; isopropyl alcohol

1N-HCl: 1N-HCl

: 170791-09-0
cilexetil trityl candesartan

: 145040-37-5
candesartan cilexetil

Conditions

Conditions	Yield
With sodium bicarbonate In methanol; dichloromethane; water; ethyl acetate	75%

: 139481-72-4
2-Ethoxy-1-[[2'-(N-triphenylmethyltetrazol-5-yl)-biphenyl-4-yl]methyl]benzimidazole-7-carboxylic acid

: 145040-37-5
candesartan cilexetil

Conditions

Conditions	Yield
With water In methanol; toluene for 2 - 4h; Product distribution / selectivity; Heating / reflux;	67%

: 1307853-79-7
C41H42N6O7

: 145040-37-5
candesartan cilexetil

Conditions

Conditions	Yield
With ammonium formate; 5%-palladium/activated carbon In water; isopropyl alcohol at 40 - 50℃; for 17h;	55%

: 139481-72-4
2-Ethoxy-1-[[2'-(N-triphenylmethyltetrazol-5-yl)-biphenyl-4-yl]methyl]benzimidazole-7-carboxylic acid

1N-HCl: 1N-HCl

: 95789-69-8, 102672-57-1
cyclohexyl (1-iodoethyl)carbonate

: 145040-37-5
candesartan cilexetil

Conditions

Conditions	Yield
With potassium carbonate In methanol; ethanol; water; N,N-dimethyl-formamide

...Expand

methanolic hydrogen chloride: methanolic hydrogen chloride

: 170791-09-0
cilexetil trityl candesartan

: 111-87-5
octanol

: 145040-37-5
candesartan cilexetil

Conditions

Conditions	Yield
With hydrogenchloride In methanol; ethanol; hexane; dichloromethane; water; acetone

...Expand

: 170791-09-0
cilexetil trityl candesartan

A: 869631-11-8
(1RS)-1-[[(cyclohexyloxy)carbonyl]oxy]ethyl 2-oxo-3-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-2,3-dihydro-1H-benzimidazole-4-carboxylate

B: 145040-37-5
candesartan cilexetil

Conditions

Conditions	Yield
With methanol for 24h; Product distribution / selectivity; Heating / reflux;
With methanol; formic acid In dichloromethane at 25℃; for 5 - 23h; Product distribution / selectivity;
Stage #1: cilexetil trityl candesartan With methanol; water; zinc(II) chloride for 2.5h; Heating / reflux; Stage #2: With water; sodium hydrogencarbonate In methanol at 20℃; pH=6.11; Product distribution / selectivity;

: 632322-62-4
2-ethoxy-1-[(2'-cyanobiphenyl-4-yl)methyl]-1H-benzimidazole-7-carboxylicacid-1-[[(cyclohexyloxy)carbonyl]oxy]ethyl ester

: 145040-37-5
candesartan cilexetil

Conditions

Conditions	Yield
With azido tributyltin (IV) In toluene for 52.5h; Heating / reflux;

: 99464-83-2
1-chloroethyl cyclohexyl carbonate

: 18162-48-6
tert-butyldimethylsilyl chloride

: 139481-59-7
candesartan

: 145040-37-5
candesartan cilexetil

Conditions

Conditions	Yield
Stage #1: tert-butyldimethylsilyl chloride; candesartan With triethylamine In chloroform at 20℃; for 3h; Stage #2: 1-chloroethyl cyclohexyl carbonate With triethylamine In chloroform for 24h;

...Expand

: 139481-59-7
candesartan

: 145040-37-5
candesartan cilexetil

Conditions

Conditions	Yield
Multi-step reaction with 3 steps 1.1: triethylamine / dichloromethane / 3.75 h / 25 - 35 °C 2.1: potassium carbonate / N,N-dimethyl-formamide / 2.5 h / 60 - 65 °C 3.1: formic acid; methanol / dichloromethane / 7 h / 30 - 35 °C 3.2: 0.33 h / 15 - 20 °C View Scheme
Multi-step reaction with 3 steps 1: triethylamine / dichloromethane / 8 h / 0 - 20 °C 2: potassium carbonate; potassium iodide / N,N-dimethyl-formamide / 2 h / 75 °C 3: hydrogen / palladium 10% on activated carbon / toluene; methanol / 20 °C / 2280.15 Torr View Scheme
Multi-step reaction with 3 steps 1: triethylamine / dichloromethane / 3.5 h / 15 - 23 °C / Flow reactor; Large scale 2: potassium carbonate / N,N-dimethyl-formamide / 4 h / 60 °C / Flow reactor; Alkaline conditions; Large scale 3: hydrogenchloride / dichloromethane; methanol / -14 - -12 °C / Flow reactor; Large scale View Scheme

: 21606-04-2
methyl 2-carboxy-3-nitrobenzoate

: 145040-37-5
candesartan cilexetil

Conditions

Conditions	Yield
Multi-step reaction with 10 steps 1.1: N,N-dimethyl-formamide; thionyl chloride / toluene / 2.5 h / 75 °C 2.1: sodium azide; tetrabutylammomium bromide / toluene / 4 h / -10 - -5 °C 2.2: 1 h / 80 - 85 °C 3.1: potassium carbonate; tetrabutylammomium bromide / toluene / 12 h / 80 - 85 °C 3.2: 3 h / Reflux 4.1: tin(ll) chloride / ethyl acetate / 1.5 h / Reflux 4.2: 4.5 h / -10 - 0 °C 4.3: 0.5 h / Reflux 5.1: acetic acid / toluene / 6 h / Reflux 6.1: sodium azide; tributyltin chloride / toluene / 100 h / Reflux 6.2: 0 - 20 °C 7.1: sodium hydroxide; water / ethanol / 3.5 h / Reflux 7.2: 3 h / 0 °C / pH 4 8.1: triethylamine / dichloromethane / 8 h / 0 - 20 °C 9.1: potassium carbonate; potassium iodide / N,N-dimethyl-formamide / 2 h / 75 °C 10.1: hydrogen / palladium 10% on activated carbon / toluene; methanol / 20 °C / 2280.15 Torr View Scheme
Multi-step reaction with 8 steps 1.1: triethylamine; diphenyl phosphoryl azide / N,N-dimethyl-formamide / 20 - 31 °C / Inert atmosphere 1.2: 9 h / 85 - 87 °C 1.3: 3 h / 50 - 55 °C 2.1: potassium carbonate / acetonitrile / 6 h / Reflux; Inert atmosphere 3.1: hydrogenchloride / methanol / 3.22 h / 3 - 9 °C 4.1: tin(II) chloride dihdyrate / methanol / 2 h / Reflux 5.1: acetic acid / 1 h / 90 °C 6.1: sodium hydroxide / methanol / 2 h / 90 °C 7.1: potassium carbonate / N,N-dimethyl-formamide / 4 h / 65 °C 8.1: ammonium formate / 5%-palladium/activated carbon / isopropyl alcohol; water / 17 h / 40 - 50 °C View Scheme

Yield

Multi-step reaction with 10 steps
1.1: N,N-dimethyl-formamide; thionyl chloride / toluene / 2.5 h / 75 °C
2.1: sodium azide; tetrabutylammomium bromide / toluene / 4 h / -10 - -5 °C
2.2: 1 h / 80 - 85 °C
3.1: potassium carbonate; tetrabutylammomium bromide / toluene / 12 h / 80 - 85 °C
3.2: 3 h / Reflux
4.1: tin(ll) chloride / ethyl acetate / 1.5 h / Reflux
4.2: 4.5 h / -10 - 0 °C
4.3: 0.5 h / Reflux
5.1: acetic acid / toluene / 6 h / Reflux
6.1: sodium azide; tributyltin chloride / toluene / 100 h / Reflux
6.2: 0 - 20 °C
7.1: sodium hydroxide; water / ethanol / 3.5 h / Reflux
7.2: 3 h / 0 °C / pH 4
8.1: triethylamine / dichloromethane / 8 h / 0 - 20 °C
9.1: potassium carbonate; potassium iodide / N,N-dimethyl-formamide / 2 h / 75 °C
10.1: hydrogen / palladium 10% on activated carbon / toluene; methanol / 20 °C / 2280.15 Torr
View Scheme

Multi-step reaction with 8 steps
1.1: triethylamine; diphenyl phosphoryl azide / N,N-dimethyl-formamide / 20 - 31 °C / Inert atmosphere
1.2: 9 h / 85 - 87 °C
1.3: 3 h / 50 - 55 °C
2.1: potassium carbonate / acetonitrile / 6 h / Reflux; Inert atmosphere
3.1: hydrogenchloride / methanol / 3.22 h / 3 - 9 °C
4.1: tin(II) chloride dihdyrate / methanol / 2 h / Reflux
5.1: acetic acid / 1 h / 90 °C
6.1: sodium hydroxide / methanol / 2 h / 90 °C
7.1: potassium carbonate / N,N-dimethyl-formamide / 4 h / 65 °C
8.1: ammonium formate / 5%-palladium/activated carbon / isopropyl alcohol; water / 17 h / 40 - 50 °C
View Scheme

: 57113-90-3
methyl 2-(N-tert-butoxycarbonylamino)-3-nitrobenzoate

: 145040-37-5
candesartan cilexetil

Conditions

Conditions	Yield
Multi-step reaction with 8 steps 1.1: potassium carbonate; tetrabutylammomium bromide / toluene / 12 h / 80 - 85 °C 1.2: 3 h / Reflux 2.1: tin(ll) chloride / ethyl acetate / 1.5 h / Reflux 2.2: 4.5 h / -10 - 0 °C 2.3: 0.5 h / Reflux 3.1: acetic acid / toluene / 6 h / Reflux 4.1: sodium azide; tributyltin chloride / toluene / 100 h / Reflux 4.2: 0 - 20 °C 5.1: sodium hydroxide; water / ethanol / 3.5 h / Reflux 5.2: 3 h / 0 °C / pH 4 6.1: triethylamine / dichloromethane / 8 h / 0 - 20 °C 7.1: potassium carbonate; potassium iodide / N,N-dimethyl-formamide / 2 h / 75 °C 8.1: hydrogen / palladium 10% on activated carbon / toluene; methanol / 20 °C / 2280.15 Torr View Scheme
Multi-step reaction with 7 steps 1: potassium carbonate / acetonitrile / 6 h / Reflux; Inert atmosphere 2: hydrogenchloride / methanol / 3.22 h / 3 - 9 °C 3: tin(II) chloride dihdyrate / methanol / 2 h / Reflux 4: acetic acid / 1 h / 90 °C 5: sodium hydroxide / methanol / 2 h / 90 °C 6: potassium carbonate / N,N-dimethyl-formamide / 4 h / 65 °C 7: ammonium formate / 5%-palladium/activated carbon / isopropyl alcohol; water / 17 h / 40 - 50 °C View Scheme

Yield

Multi-step reaction with 8 steps
1.1: potassium carbonate; tetrabutylammomium bromide / toluene / 12 h / 80 - 85 °C
1.2: 3 h / Reflux
2.1: tin(ll) chloride / ethyl acetate / 1.5 h / Reflux
2.2: 4.5 h / -10 - 0 °C
2.3: 0.5 h / Reflux
3.1: acetic acid / toluene / 6 h / Reflux
4.1: sodium azide; tributyltin chloride / toluene / 100 h / Reflux
4.2: 0 - 20 °C
5.1: sodium hydroxide; water / ethanol / 3.5 h / Reflux
5.2: 3 h / 0 °C / pH 4
6.1: triethylamine / dichloromethane / 8 h / 0 - 20 °C
7.1: potassium carbonate; potassium iodide / N,N-dimethyl-formamide / 2 h / 75 °C
8.1: hydrogen / palladium 10% on activated carbon / toluene; methanol / 20 °C / 2280.15 Torr
View Scheme

Multi-step reaction with 7 steps
1: potassium carbonate / acetonitrile / 6 h / Reflux; Inert atmosphere
2: hydrogenchloride / methanol / 3.22 h / 3 - 9 °C
3: tin(II) chloride dihdyrate / methanol / 2 h / Reflux
4: acetic acid / 1 h / 90 °C
5: sodium hydroxide / methanol / 2 h / 90 °C
6: potassium carbonate / N,N-dimethyl-formamide / 4 h / 65 °C
7: ammonium formate / 5%-palladium/activated carbon / isopropyl alcohol; water / 17 h / 40 - 50 °C
View Scheme

: 139481-69-9
methyl 2-ethoxy-1-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]benzimidazole-7-carboxylate

: 145040-37-5
candesartan cilexetil

Conditions

Conditions	Yield
Multi-step reaction with 4 steps 1.1: sodium hydroxide; water / ethanol / 3.5 h / Reflux 1.2: 3 h / 0 °C / pH 4 2.1: triethylamine / dichloromethane / 8 h / 0 - 20 °C 3.1: potassium carbonate; potassium iodide / N,N-dimethyl-formamide / 2 h / 75 °C 4.1: hydrogen / palladium 10% on activated carbon / toluene; methanol / 20 °C / 2280.15 Torr View Scheme

: 136304-78-4
methyl 3-amino-2-[[(2'-cyanobiphenyl-4-yl)methyl]amino]benzoate

: 145040-37-5
candesartan cilexetil

Conditions

Conditions	Yield
Multi-step reaction with 6 steps 1.1: acetic acid / toluene / 6 h / Reflux 2.1: sodium azide; tributyltin chloride / toluene / 100 h / Reflux 2.2: 0 - 20 °C 3.1: sodium hydroxide; water / ethanol / 3.5 h / Reflux 3.2: 3 h / 0 °C / pH 4 4.1: triethylamine / dichloromethane / 8 h / 0 - 20 °C 5.1: potassium carbonate; potassium iodide / N,N-dimethyl-formamide / 2 h / 75 °C 6.1: hydrogen / palladium 10% on activated carbon / toluene; methanol / 20 °C / 2280.15 Torr View Scheme

Yield

Multi-step reaction with 6 steps
1.1: acetic acid / toluene / 6 h / Reflux
2.1: sodium azide; tributyltin chloride / toluene / 100 h / Reflux
2.2: 0 - 20 °C
3.1: sodium hydroxide; water / ethanol / 3.5 h / Reflux
3.2: 3 h / 0 °C / pH 4
4.1: triethylamine / dichloromethane / 8 h / 0 - 20 °C
5.1: potassium carbonate; potassium iodide / N,N-dimethyl-formamide / 2 h / 75 °C
6.1: hydrogen / palladium 10% on activated carbon / toluene; methanol / 20 °C / 2280.15 Torr
View Scheme

: 603-11-2
3-nitrophthalic acid

: 145040-37-5
candesartan cilexetil

Conditions

Conditions	Yield
Multi-step reaction with 11 steps 1.1: sulfuric acid / 24.75 h / 20 - 65 °C 2.1: N,N-dimethyl-formamide; thionyl chloride / toluene / 2.5 h / 75 °C 3.1: sodium azide; tetrabutylammomium bromide / toluene / 4 h / -10 - -5 °C 3.2: 1 h / 80 - 85 °C 4.1: potassium carbonate; tetrabutylammomium bromide / toluene / 12 h / 80 - 85 °C 4.2: 3 h / Reflux 5.1: tin(ll) chloride / ethyl acetate / 1.5 h / Reflux 5.2: 4.5 h / -10 - 0 °C 5.3: 0.5 h / Reflux 6.1: acetic acid / toluene / 6 h / Reflux 7.1: sodium azide; tributyltin chloride / toluene / 100 h / Reflux 7.2: 0 - 20 °C 8.1: sodium hydroxide; water / ethanol / 3.5 h / Reflux 8.2: 3 h / 0 °C / pH 4 9.1: triethylamine / dichloromethane / 8 h / 0 - 20 °C 10.1: potassium carbonate; potassium iodide / N,N-dimethyl-formamide / 2 h / 75 °C 11.1: hydrogen / palladium 10% on activated carbon / toluene; methanol / 20 °C / 2280.15 Torr View Scheme

Yield

Multi-step reaction with 11 steps
1.1: sulfuric acid / 24.75 h / 20 - 65 °C
2.1: N,N-dimethyl-formamide; thionyl chloride / toluene / 2.5 h / 75 °C
3.1: sodium azide; tetrabutylammomium bromide / toluene / 4 h / -10 - -5 °C
3.2: 1 h / 80 - 85 °C
4.1: potassium carbonate; tetrabutylammomium bromide / toluene / 12 h / 80 - 85 °C
4.2: 3 h / Reflux
5.1: tin(ll) chloride / ethyl acetate / 1.5 h / Reflux
5.2: 4.5 h / -10 - 0 °C
5.3: 0.5 h / Reflux
6.1: acetic acid / toluene / 6 h / Reflux
7.1: sodium azide; tributyltin chloride / toluene / 100 h / Reflux
7.2: 0 - 20 °C
8.1: sodium hydroxide; water / ethanol / 3.5 h / Reflux
8.2: 3 h / 0 °C / pH 4
9.1: triethylamine / dichloromethane / 8 h / 0 - 20 °C
10.1: potassium carbonate; potassium iodide / N,N-dimethyl-formamide / 2 h / 75 °C
11.1: hydrogen / palladium 10% on activated carbon / toluene; methanol / 20 °C / 2280.15 Torr
View Scheme

: 139481-28-0
methyl 2-<<2'-cyanobiphenyl-4-yl)methyl>amino>-3-nitrobenzoate

: 145040-37-5
candesartan cilexetil

Conditions

Conditions	Yield
Multi-step reaction with 7 steps 1.1: tin(ll) chloride / ethyl acetate / 1.5 h / Reflux 1.2: 4.5 h / -10 - 0 °C 1.3: 0.5 h / Reflux 2.1: acetic acid / toluene / 6 h / Reflux 3.1: sodium azide; tributyltin chloride / toluene / 100 h / Reflux 3.2: 0 - 20 °C 4.1: sodium hydroxide; water / ethanol / 3.5 h / Reflux 4.2: 3 h / 0 °C / pH 4 5.1: triethylamine / dichloromethane / 8 h / 0 - 20 °C 6.1: potassium carbonate; potassium iodide / N,N-dimethyl-formamide / 2 h / 75 °C 7.1: hydrogen / palladium 10% on activated carbon / toluene; methanol / 20 °C / 2280.15 Torr View Scheme

Yield

Multi-step reaction with 7 steps
1.1: tin(ll) chloride / ethyl acetate / 1.5 h / Reflux
1.2: 4.5 h / -10 - 0 °C
1.3: 0.5 h / Reflux
2.1: acetic acid / toluene / 6 h / Reflux
3.1: sodium azide; tributyltin chloride / toluene / 100 h / Reflux
3.2: 0 - 20 °C
4.1: sodium hydroxide; water / ethanol / 3.5 h / Reflux
4.2: 3 h / 0 °C / pH 4
5.1: triethylamine / dichloromethane / 8 h / 0 - 20 °C
6.1: potassium carbonate; potassium iodide / N,N-dimethyl-formamide / 2 h / 75 °C
7.1: hydrogen / palladium 10% on activated carbon / toluene; methanol / 20 °C / 2280.15 Torr
View Scheme

: 73833-13-3
acid chloride of 1-methylhydrogen-3-nitrophthalate

: 145040-37-5
candesartan cilexetil

Conditions

Conditions	Yield
Multi-step reaction with 9 steps 1.1: sodium azide; tetrabutylammomium bromide / toluene / 4 h / -10 - -5 °C 1.2: 1 h / 80 - 85 °C 2.1: potassium carbonate; tetrabutylammomium bromide / toluene / 12 h / 80 - 85 °C 2.2: 3 h / Reflux 3.1: tin(ll) chloride / ethyl acetate / 1.5 h / Reflux 3.2: 4.5 h / -10 - 0 °C 3.3: 0.5 h / Reflux 4.1: acetic acid / toluene / 6 h / Reflux 5.1: sodium azide; tributyltin chloride / toluene / 100 h / Reflux 5.2: 0 - 20 °C 6.1: sodium hydroxide; water / ethanol / 3.5 h / Reflux 6.2: 3 h / 0 °C / pH 4 7.1: triethylamine / dichloromethane / 8 h / 0 - 20 °C 8.1: potassium carbonate; potassium iodide / N,N-dimethyl-formamide / 2 h / 75 °C 9.1: hydrogen / palladium 10% on activated carbon / toluene; methanol / 20 °C / 2280.15 Torr View Scheme

Yield

Multi-step reaction with 9 steps
1.1: sodium azide; tetrabutylammomium bromide / toluene / 4 h / -10 - -5 °C
1.2: 1 h / 80 - 85 °C
2.1: potassium carbonate; tetrabutylammomium bromide / toluene / 12 h / 80 - 85 °C
2.2: 3 h / Reflux
3.1: tin(ll) chloride / ethyl acetate / 1.5 h / Reflux
3.2: 4.5 h / -10 - 0 °C
3.3: 0.5 h / Reflux
4.1: acetic acid / toluene / 6 h / Reflux
5.1: sodium azide; tributyltin chloride / toluene / 100 h / Reflux
5.2: 0 - 20 °C
6.1: sodium hydroxide; water / ethanol / 3.5 h / Reflux
6.2: 3 h / 0 °C / pH 4
7.1: triethylamine / dichloromethane / 8 h / 0 - 20 °C
8.1: potassium carbonate; potassium iodide / N,N-dimethyl-formamide / 2 h / 75 °C
9.1: hydrogen / palladium 10% on activated carbon / toluene; methanol / 20 °C / 2280.15 Torr
View Scheme

: methyl 1-[(2-cyanobiphenyl-4-yl)methyl]-2-ethoxybenzimidazole-7-carboxylate

: 145040-37-5
candesartan cilexetil

Conditions

Conditions	Yield
Multi-step reaction with 5 steps 1.1: sodium azide; tributyltin chloride / toluene / 100 h / Reflux 1.2: 0 - 20 °C 2.1: sodium hydroxide; water / ethanol / 3.5 h / Reflux 2.2: 3 h / 0 °C / pH 4 3.1: triethylamine / dichloromethane / 8 h / 0 - 20 °C 4.1: potassium carbonate; potassium iodide / N,N-dimethyl-formamide / 2 h / 75 °C 5.1: hydrogen / palladium 10% on activated carbon / toluene; methanol / 20 °C / 2280.15 Torr View Scheme

Yield

Multi-step reaction with 5 steps
1.1: sodium azide; tributyltin chloride / toluene / 100 h / Reflux
1.2: 0 - 20 °C
2.1: sodium hydroxide; water / ethanol / 3.5 h / Reflux
2.2: 3 h / 0 °C / pH 4
3.1: triethylamine / dichloromethane / 8 h / 0 - 20 °C
4.1: potassium carbonate; potassium iodide / N,N-dimethyl-formamide / 2 h / 75 °C
5.1: hydrogen / palladium 10% on activated carbon / toluene; methanol / 20 °C / 2280.15 Torr
View Scheme

: 1-(cyclohexyloxycarbonyloxy)ethyl 2-ethoxy-1-[[2'-(N-triphenylmethyltetrazole-5-yl)biphenyl-4-yl]methyl]benzimidazole-7-carboxylate

: 145040-37-5
candesartan cilexetil

Conditions

Conditions	Yield
With hydrogen; palladium 10% on activated carbon In methanol; toluene at 20℃; under 2280.15 Torr; Product distribution / selectivity;

: 98-88-4
benzoyl chloride

: 145040-37-5
candesartan cilexetil

Conditions

Conditions	Yield
Multi-step reaction with 12 steps 1.1: triethylamine / tetrahydrofuran / 7 - 16 °C 2.1: phosphorus pentachloride / dichloromethane / -11 - 19 °C 2.2: 7 h / -6 - 20 °C 3.1: potassium carbonate; triphenylphosphine / dichloro(1,5-cyclooctadiene)ruthenium(II) polymer / 1-methyl-pyrrolidin-2-one / 2 h / 140 °C / Inert atmosphere 4.1: sodium methylate / methanol / 1.5 h / 20 °C 5.1: phosphorus tribromide / tetrahydrofuran / 5.5 h / 0 - 20 °C 6.1: potassium carbonate / acetonitrile / 6 h / Reflux; Inert atmosphere 7.1: hydrogenchloride / methanol / 3.22 h / 3 - 9 °C 8.1: tin(II) chloride dihdyrate / methanol / 2 h / Reflux 9.1: acetic acid / 1 h / 90 °C 10.1: sodium hydroxide / methanol / 2 h / 90 °C 11.1: potassium carbonate / N,N-dimethyl-formamide / 4 h / 65 °C 12.1: ammonium formate / 5%-palladium/activated carbon / isopropyl alcohol; water / 17 h / 40 - 50 °C View Scheme

Yield

Multi-step reaction with 12 steps
1.1: triethylamine / tetrahydrofuran / 7 - 16 °C
2.1: phosphorus pentachloride / dichloromethane / -11 - 19 °C
2.2: 7 h / -6 - 20 °C
3.1: potassium carbonate; triphenylphosphine / dichloro(1,5-cyclooctadiene)ruthenium(II) polymer / 1-methyl-pyrrolidin-2-one / 2 h / 140 °C / Inert atmosphere
4.1: sodium methylate / methanol / 1.5 h / 20 °C
5.1: phosphorus tribromide / tetrahydrofuran / 5.5 h / 0 - 20 °C
6.1: potassium carbonate / acetonitrile / 6 h / Reflux; Inert atmosphere
7.1: hydrogenchloride / methanol / 3.22 h / 3 - 9 °C
8.1: tin(II) chloride dihdyrate / methanol / 2 h / Reflux
9.1: acetic acid / 1 h / 90 °C
10.1: sodium hydroxide / methanol / 2 h / 90 °C
11.1: potassium carbonate / N,N-dimethyl-formamide / 4 h / 65 °C
12.1: ammonium formate / 5%-palladium/activated carbon / isopropyl alcohol; water / 17 h / 40 - 50 °C
View Scheme

: 21388-92-1
4-bromobenzyl acetate

: 145040-37-5
candesartan cilexetil

Conditions

Conditions	Yield
Multi-step reaction with 10 steps 1: potassium carbonate; triphenylphosphine / dichloro(1,5-cyclooctadiene)ruthenium(II) polymer / 1-methyl-pyrrolidin-2-one / 2 h / 140 °C / Inert atmosphere 2: sodium methylate / methanol / 1.5 h / 20 °C 3: phosphorus tribromide / tetrahydrofuran / 5.5 h / 0 - 20 °C 4: potassium carbonate / acetonitrile / 6 h / Reflux; Inert atmosphere 5: hydrogenchloride / methanol / 3.22 h / 3 - 9 °C 6: tin(II) chloride dihdyrate / methanol / 2 h / Reflux 7: acetic acid / 1 h / 90 °C 8: sodium hydroxide / methanol / 2 h / 90 °C 9: potassium carbonate / N,N-dimethyl-formamide / 4 h / 65 °C 10: ammonium formate / 5%-palladium/activated carbon / isopropyl alcohol; water / 17 h / 40 - 50 °C View Scheme

Yield

Multi-step reaction with 10 steps
1: potassium carbonate; triphenylphosphine / dichloro(1,5-cyclooctadiene)ruthenium(II) polymer / 1-methyl-pyrrolidin-2-one / 2 h / 140 °C / Inert atmosphere
2: sodium methylate / methanol / 1.5 h / 20 °C
3: phosphorus tribromide / tetrahydrofuran / 5.5 h / 0 - 20 °C
4: potassium carbonate / acetonitrile / 6 h / Reflux; Inert atmosphere
5: hydrogenchloride / methanol / 3.22 h / 3 - 9 °C
6: tin(II) chloride dihdyrate / methanol / 2 h / Reflux
7: acetic acid / 1 h / 90 °C
8: sodium hydroxide / methanol / 2 h / 90 °C
9: potassium carbonate / N,N-dimethyl-formamide / 4 h / 65 °C
10: ammonium formate / 5%-palladium/activated carbon / isopropyl alcohol; water / 17 h / 40 - 50 °C
View Scheme

: 873-75-6
4-bromobenzenemethanol

: 145040-37-5
candesartan cilexetil

Conditions

Conditions	Yield
Multi-step reaction with 11 steps 1: dmap; triethylamine / tetrahydrofuran / 15 - 30 °C 2: potassium carbonate; triphenylphosphine / dichloro(1,5-cyclooctadiene)ruthenium(II) polymer / 1-methyl-pyrrolidin-2-one / 2 h / 140 °C / Inert atmosphere 3: sodium methylate / methanol / 1.5 h / 20 °C 4: phosphorus tribromide / tetrahydrofuran / 5.5 h / 0 - 20 °C 5: potassium carbonate / acetonitrile / 6 h / Reflux; Inert atmosphere 6: hydrogenchloride / methanol / 3.22 h / 3 - 9 °C 7: tin(II) chloride dihdyrate / methanol / 2 h / Reflux 8: acetic acid / 1 h / 90 °C 9: sodium hydroxide / methanol / 2 h / 90 °C 10: potassium carbonate / N,N-dimethyl-formamide / 4 h / 65 °C 11: ammonium formate / 5%-palladium/activated carbon / isopropyl alcohol; water / 17 h / 40 - 50 °C View Scheme

Yield

Multi-step reaction with 11 steps
1: dmap; triethylamine / tetrahydrofuran / 15 - 30 °C
2: potassium carbonate; triphenylphosphine / dichloro(1,5-cyclooctadiene)ruthenium(II) polymer / 1-methyl-pyrrolidin-2-one / 2 h / 140 °C / Inert atmosphere
3: sodium methylate / methanol / 1.5 h / 20 °C
4: phosphorus tribromide / tetrahydrofuran / 5.5 h / 0 - 20 °C
5: potassium carbonate / acetonitrile / 6 h / Reflux; Inert atmosphere
6: hydrogenchloride / methanol / 3.22 h / 3 - 9 °C
7: tin(II) chloride dihdyrate / methanol / 2 h / Reflux
8: acetic acid / 1 h / 90 °C
9: sodium hydroxide / methanol / 2 h / 90 °C
10: potassium carbonate / N,N-dimethyl-formamide / 4 h / 65 °C
11: ammonium formate / 5%-palladium/activated carbon / isopropyl alcohol; water / 17 h / 40 - 50 °C
View Scheme

: 18039-42-4
5-Phenyl-1H-tetrazole

: 145040-37-5
candesartan cilexetil

Conditions

Conditions	Yield
Multi-step reaction with 11 steps 1.1: sodium carbonate; tetrabutylammomium bromide / chloroform; water / 2 h / 55 °C / Cooling with ice 1.2: 1 h 2.1: potassium carbonate; triphenylphosphine / dichloro(1,5-cyclooctadiene)ruthenium(II) polymer / 1-methyl-pyrrolidin-2-one / 2 h / 140 °C / Inert atmosphere 3.1: sodium methylate / methanol / 1.5 h / 20 °C 4.1: phosphorus tribromide / tetrahydrofuran / 5.5 h / 0 - 20 °C 5.1: potassium carbonate / acetonitrile / 6 h / Reflux; Inert atmosphere 6.1: hydrogenchloride / methanol / 3.22 h / 3 - 9 °C 7.1: tin(II) chloride dihdyrate / methanol / 2 h / Reflux 8.1: acetic acid / 1 h / 90 °C 9.1: sodium hydroxide / methanol / 2 h / 90 °C 10.1: potassium carbonate / N,N-dimethyl-formamide / 4 h / 65 °C 11.1: ammonium formate / 5%-palladium/activated carbon / isopropyl alcohol; water / 17 h / 40 - 50 °C View Scheme
Multi-step reaction with 11 steps 1: sodium carbonate; tetrabutylammomium bromide / chloroform; water / 2 h / 55 °C / Cooling with ice 2: potassium carbonate; triphenylphosphine / dichloro(1,5-cyclooctadiene)ruthenium(II) polymer / 1-methyl-pyrrolidin-2-one / 2 h / 140 °C / Inert atmosphere 3: sodium methylate / methanol / 1.5 h / 20 °C 4: phosphorus tribromide / tetrahydrofuran / 5.5 h / 0 - 20 °C 5: potassium carbonate / acetonitrile / 6 h / Reflux; Inert atmosphere 6: hydrogenchloride / methanol / 3.22 h / 3 - 9 °C 7: tin(II) chloride dihdyrate / methanol / 2 h / Reflux 8: acetic acid / 1 h / 90 °C 9: sodium hydroxide / methanol / 2 h / 90 °C 10: potassium carbonate / N,N-dimethyl-formamide / 4 h / 65 °C 11: ammonium formate / 5%-palladium/activated carbon / isopropyl alcohol; water / 17 h / 40 - 50 °C View Scheme

Yield

Multi-step reaction with 11 steps
1.1: sodium carbonate; tetrabutylammomium bromide / chloroform; water / 2 h / 55 °C / Cooling with ice
1.2: 1 h
2.1: potassium carbonate; triphenylphosphine / dichloro(1,5-cyclooctadiene)ruthenium(II) polymer / 1-methyl-pyrrolidin-2-one / 2 h / 140 °C / Inert atmosphere
3.1: sodium methylate / methanol / 1.5 h / 20 °C
4.1: phosphorus tribromide / tetrahydrofuran / 5.5 h / 0 - 20 °C
5.1: potassium carbonate / acetonitrile / 6 h / Reflux; Inert atmosphere
6.1: hydrogenchloride / methanol / 3.22 h / 3 - 9 °C
7.1: tin(II) chloride dihdyrate / methanol / 2 h / Reflux
8.1: acetic acid / 1 h / 90 °C
9.1: sodium hydroxide / methanol / 2 h / 90 °C
10.1: potassium carbonate / N,N-dimethyl-formamide / 4 h / 65 °C
11.1: ammonium formate / 5%-palladium/activated carbon / isopropyl alcohol; water / 17 h / 40 - 50 °C
View Scheme

Multi-step reaction with 11 steps
1: sodium carbonate; tetrabutylammomium bromide / chloroform; water / 2 h / 55 °C / Cooling with ice
2: potassium carbonate; triphenylphosphine / dichloro(1,5-cyclooctadiene)ruthenium(II) polymer / 1-methyl-pyrrolidin-2-one / 2 h / 140 °C / Inert atmosphere
3: sodium methylate / methanol / 1.5 h / 20 °C
4: phosphorus tribromide / tetrahydrofuran / 5.5 h / 0 - 20 °C
5: potassium carbonate / acetonitrile / 6 h / Reflux; Inert atmosphere
6: hydrogenchloride / methanol / 3.22 h / 3 - 9 °C
7: tin(II) chloride dihdyrate / methanol / 2 h / Reflux
8: acetic acid / 1 h / 90 °C
9: sodium hydroxide / methanol / 2 h / 90 °C
10: potassium carbonate / N,N-dimethyl-formamide / 4 h / 65 °C
11: ammonium formate / 5%-palladium/activated carbon / isopropyl alcohol; water / 17 h / 40 - 50 °C
View Scheme

: 512182-38-6
1-(p-methoxybenzyl)-5-phenyl-1H-tetrazole

: 145040-37-5
candesartan cilexetil

Conditions

Conditions	Yield
Multi-step reaction with 10 steps 1: potassium carbonate; triphenylphosphine / dichloro(1,5-cyclooctadiene)ruthenium(II) polymer / 1-methyl-pyrrolidin-2-one / 2 h / 140 °C / Inert atmosphere 2: sodium methylate / methanol / 1.5 h / 20 °C 3: phosphorus tribromide / tetrahydrofuran / 5.5 h / 0 - 20 °C 4: potassium carbonate / acetonitrile / 6 h / Reflux; Inert atmosphere 5: hydrogenchloride / methanol / 3.22 h / 3 - 9 °C 6: tin(II) chloride dihdyrate / methanol / 2 h / Reflux 7: acetic acid / 1 h / 90 °C 8: sodium hydroxide / methanol / 2 h / 90 °C 9: potassium carbonate / N,N-dimethyl-formamide / 4 h / 65 °C 10: ammonium formate / 5%-palladium/activated carbon / isopropyl alcohol; water / 17 h / 40 - 50 °C View Scheme

Yield

: 41882-10-4
N-(4-methoxybenzyl)benzamide

: 145040-37-5
candesartan cilexetil

Conditions

Conditions	Yield
Multi-step reaction with 11 steps 1.1: phosphorus pentachloride / dichloromethane / -11 - 19 °C 1.2: 7 h / -6 - 20 °C 2.1: potassium carbonate; triphenylphosphine / dichloro(1,5-cyclooctadiene)ruthenium(II) polymer / 1-methyl-pyrrolidin-2-one / 2 h / 140 °C / Inert atmosphere 3.1: sodium methylate / methanol / 1.5 h / 20 °C 4.1: phosphorus tribromide / tetrahydrofuran / 5.5 h / 0 - 20 °C 5.1: potassium carbonate / acetonitrile / 6 h / Reflux; Inert atmosphere 6.1: hydrogenchloride / methanol / 3.22 h / 3 - 9 °C 7.1: tin(II) chloride dihdyrate / methanol / 2 h / Reflux 8.1: acetic acid / 1 h / 90 °C 9.1: sodium hydroxide / methanol / 2 h / 90 °C 10.1: potassium carbonate / N,N-dimethyl-formamide / 4 h / 65 °C 11.1: ammonium formate / 5%-palladium/activated carbon / isopropyl alcohol; water / 17 h / 40 - 50 °C View Scheme

Yield

Multi-step reaction with 11 steps
1.1: phosphorus pentachloride / dichloromethane / -11 - 19 °C
1.2: 7 h / -6 - 20 °C
2.1: potassium carbonate; triphenylphosphine / dichloro(1,5-cyclooctadiene)ruthenium(II) polymer / 1-methyl-pyrrolidin-2-one / 2 h / 140 °C / Inert atmosphere
3.1: sodium methylate / methanol / 1.5 h / 20 °C
4.1: phosphorus tribromide / tetrahydrofuran / 5.5 h / 0 - 20 °C
5.1: potassium carbonate / acetonitrile / 6 h / Reflux; Inert atmosphere
6.1: hydrogenchloride / methanol / 3.22 h / 3 - 9 °C
7.1: tin(II) chloride dihdyrate / methanol / 2 h / Reflux
8.1: acetic acid / 1 h / 90 °C
9.1: sodium hydroxide / methanol / 2 h / 90 °C
10.1: potassium carbonate / N,N-dimethyl-formamide / 4 h / 65 °C
11.1: ammonium formate / 5%-palladium/activated carbon / isopropyl alcohol; water / 17 h / 40 - 50 °C
View Scheme

: 1307853-40-2
5-[4'-(bromomethyl)biphenyl-2-yl]-1-(p-methoxybenzyl)-1H-tetrazole

: 145040-37-5
candesartan cilexetil

Conditions

Conditions	Yield
Multi-step reaction with 7 steps 1: potassium carbonate / acetonitrile / 6 h / Reflux; Inert atmosphere 2: hydrogenchloride / methanol / 3.22 h / 3 - 9 °C 3: tin(II) chloride dihdyrate / methanol / 2 h / Reflux 4: acetic acid / 1 h / 90 °C 5: sodium hydroxide / methanol / 2 h / 90 °C 6: potassium carbonate / N,N-dimethyl-formamide / 4 h / 65 °C 7: ammonium formate / 5%-palladium/activated carbon / isopropyl alcohol; water / 17 h / 40 - 50 °C View Scheme

Yield

: 145040-37-5
candesartan cilexetil

: 869631-11-8
(1RS)-1-[[(cyclohexyloxy)carbonyl]oxy]ethyl 2-oxo-3-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-2,3-dihydro-1H-benzimidazole-4-carboxylate

Conditions

Conditions	Yield
With hydrogenchloride; water In acetone for 6h; Reflux;	87.9%

: 118457-16-2
nebivolol

: 145040-37-5
candesartan cilexetil

: candensartan cilexetil-nebivolol salt

Conditions

Conditions	Yield
In ethanol at 20 - 45℃; for 5h; Concentration; Solvent; Temperature; Time;	81%

: 145040-37-5
candesartan cilexetil

: 74-88-4
methyl iodide

: 1-(((cyclohexyloxy)carbonyl)oxy)ethyl 2-ethoxy-1-((2’-(1-methyl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate

Conditions

Conditions	Yield
In dichloromethane Reflux;	79%

: 145040-37-5
candesartan cilexetil

A: 869631-11-8
(1RS)-1-[[(cyclohexyloxy)carbonyl]oxy]ethyl 2-oxo-3-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-2,3-dihydro-1H-benzimidazole-4-carboxylate

B: 914613-35-7
(1RS)-1-[[(cyclohexyloxy)carbonyl]oxy]ethyl 2-ethoxy-1-[[2'-(1-ethyl-1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-1H-benzimidazole-7-carboxylate

C: 914613-36-8
(1RS)-1-[[(cyclohexyloxy)carbonyl]oxy]ethyl 2-ethoxy-1-[[2'-(2-ethyl-2H-tetrazol-5-yl)biphenyl-4-yl]methyl]-1H-benzimidazole-7-carboxylate

Conditions

Conditions	Yield
at 55℃; for 336h; Product distribution / selectivity;
at 55℃; for 336h; Product distribution / selectivity;

...Expand

: 145040-37-5
candesartan cilexetil

A: 869631-11-8
(1RS)-1-[[(cyclohexyloxy)carbonyl]oxy]ethyl 2-oxo-3-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-2,3-dihydro-1H-benzimidazole-4-carboxylate

B: 914613-36-8
(1RS)-1-[[(cyclohexyloxy)carbonyl]oxy]ethyl 2-ethoxy-1-[[2'-(2-ethyl-2H-tetrazol-5-yl)biphenyl-4-yl]methyl]-1H-benzimidazole-7-carboxylate

Conditions

Conditions	Yield
In ethanol at 50℃; for 31h; Product distribution / selectivity;

: 76-83-5
trityl chloride

: 145040-37-5
candesartan cilexetil

: 170791-09-0
cilexetil trityl candesartan

Conditions

Conditions	Yield
With triethylamine for 1h; Heating / reflux;

: 75-03-6
ethyl iodide

: 145040-37-5
candesartan cilexetil

A: 914613-35-7
(1RS)-1-[[(cyclohexyloxy)carbonyl]oxy]ethyl 2-ethoxy-1-[[2'-(1-ethyl-1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-1H-benzimidazole-7-carboxylate

B: 914613-36-8
(1RS)-1-[[(cyclohexyloxy)carbonyl]oxy]ethyl 2-ethoxy-1-[[2'-(2-ethyl-2H-tetrazol-5-yl)biphenyl-4-yl]methyl]-1H-benzimidazole-7-carboxylate

Conditions

Conditions	Yield
Stage #1: candesartan cilexetil With potassium carbonate In acetone at 20℃; for 1h; Inert atmosphere; Stage #2: ethyl iodide In acetone at 20℃; for 24h;	A 2.5 g B 2.9 g

...Expand

Candesartan cilexetil Specification

1. Introduction of Candesartan cilexetil
Candesartan cilexetil is one kind of white or off white powder. The IUPAC Name of it is 1-cyclohexyloxycarbonyloxyethyl 2-ethoxy-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]benzimidazole-4-carboxylate. It belongs to Antihypertensive;API;APIs;Hypertension;Bases & Related Reagents;Intermediates & Fine Chemicals;Nucleotides;Pharmaceuticals;Candesartan;Heterocycles. The Classification Code of it is Angiotensin II Type 1 Receptor Blockers; Angiotensin Receptor Antagonists; Antagonist [angiotensin II receptor]; Antihypertensive; Antihypertensive agents; Cardiovascular Agents; Drug / Therapeutic Agent.

2. Properties of Candesartan cilexetil
Physical properties about Candesartan cilexetil are:
(1)Index of Refraction: 1.666; (2)Molar Refractivity: 165.46 cm³; (3)Molar Volume: 444.6 cm³; (4)Surface Tension: 54 dyne/cm; (5)Density: 1.37 g/cm³; (6)Flash Point: 463.8 °C; (7)Enthalpy of Vaporization: 122.54 kJ/mol; (8)Boiling Point: 843.3 °C at 760 mmHg; (9)Vapour Pressure of Candesartan cilexetil: 1.11E-28 mmHg at 25 °C.

3. Structure Descriptors of Candesartan cilexetil
(1)SMILES: c1cc(c2c(c1)nc(OCC)n2Cc1ccc(cc1)c1ccccc1c1[nH]nnn1)C(O[C@@H](OC(OC1CCCCC1)=O)C)=O
(2)InChI: InChI=1/C33H34N6O6/c1-3-42-32-34-28-15-9-14-27(31(40)43-21(2)44-33(41)45-24-10-5-4-6-11-24)29(28)39(32)20-22-16-18-23(19-17-22)25-12-7-8-13-26(25)30-35-37-38-36-30/h7-9,12-19,21,24H,3-6,10-11,20H2,1-2H3,(H,35,36,37,38)
(3)InChIKey: InChIKey=GHOSNRCGJFBJIB-UHFFFAOYSA-N

4. Toxicity of Candesartan cilexetil

Organism	Test Type	Route	Reported Dose (Normalized Dose)	Effect	Source
dog	LD50	oral	> 2gm/kg (2000mg/kg)		Gekkan Yakuji. Pharmaceuticals Monthly. Vol. 42, Pg. 406, 2000.
mouse	LD50	intraperitoneal	807mg/kg (807mg/kg)	BEHAVIORAL: ALTERED SLEEP TIME (INCLUDING CHANGE IN RIGHTING REFLEX) BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY) LUNGS, THORAX, OR RESPIRATION: RESPIRATORY DEPRESSION	Yakuri to Chiryo. Pharmacology and Therapeutics. Vol. 24(Suppl,
mouse	LD50	oral	> 2gm/kg (2000mg/kg)		Yakuri to Chiryo. Pharmacology and Therapeutics. Vol. 24(Suppl,
rat	LD50	intraperitoneal	940mg/kg (940mg/kg)	BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY) BEHAVIORAL: MUSCLE WEAKNESS LUNGS, THORAX, OR RESPIRATION: RESPIRATORY DEPRESSION	Yakuri to Chiryo. Pharmacology and Therapeutics. Vol. 24(Suppl,
rat	LD50	oral	> 2gm/kg (2000mg/kg)		Yakuri to Chiryo. Pharmacology and Therapeutics. Vol. 24(Suppl,

5. Safety of Candesartan cilexetil
Hazard Codes: Harmful

Xn
Risk Statements: 20/21/22-36/37/38
R20/21/22:Harmful by inhalation, in contact with skin and if swallowed.
R36/37/38:Irritating to eyes, respiratory system and skin.
Safety Statements of Candesartan cilexetil (CAS NO.145040-37-5): 26-36
S26: In case of contact with eyes, rinse immediately with plenty of water and seek medical advice.
S36:Wear suitable protective clothing.

6. Uses of Candesartan cilexetil
Candesartan cilexetil (CAS NO.145040-37-5) is used in treatment of congestive heart failure. As an antihypertensive, it will be used in treatment of congestive heart failure.

Product Name

Candesartan cilexetil

Synthetic route

Candesartan cilexetil Specification

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