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Cas No: 116666-63-8
USD $ 3.0-3.0 / Kilogram 1 Kilogram 1-100 Metric Ton/Month Dayang Chem (Hangzhou) Co.,Ltd. Contact Supplier
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Cas No: 116666-63-8
USD $ 139.0-210.0 / Kilogram 1 Kilogram 1000 Kilogram/Day Zhuozhou Wenxi import and Export Co., Ltd Contact Supplier
Acetic acid,2-methoxy-,(1S,2S)-2-[2-[[3-(1H-benzimidazol-2-yl)propyl]methylamino]ethyl]-6-fluoro-1,2,3,4-tetrahydro-1-(1-methylethyl)-2-naphthalenylester, hydrochloride (1:2)
Cas No: 116666-63-8
No Data No Data 5 Hangzhou J&H Chemical Co., Ltd. Contact Supplier
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No Data 1 Milligram 5 Xiamen Jenny Chemical Technology Co., Ltd. Contact Supplier
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No Data 1 bottle 1 Kilogram/Day Shanghai Acmec Biochemical Technology Co., Ltd. Contact Supplier
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116666-63-8 Usage


Posicor was launched in Argentina, Azerbaijan, Brazil, the Chile, Czech Republic, Denmark, Germany, Ireland, Kazakhstan, the Netherlands, Norway, Peru, the Philippines, Switzerland, Thailand, Turkmenistan, the UK, the US and Venezuela for use in hypertension. It can be assembled in five steps from 4-(1-benzyloxy-Nmethylformamido) butyric acid with o-phenylenediamine and isobutylchloroformate. Posicor binds to calcium channels in a manner that overlaps the Verapamil, SR-33557 and Diltiazem binding site without effecting the dihydropyridine binding site. Thus it blocks a wide variety of calcium channels with selectivity for T-type followed sequentially by L-type. There is also some calcium agonist activity along with sodium and potassium channel activity. It is chemically distinct from the other calcium antagonists (first member of a new catagory of tetralol calcium antagonists). It has the ability to lower heart rate with no negative inotropic effects and is as effective as Amlodipine and more effective than Diltiazem for the treatment of mild to moderate hypertension. Serious drug interactions are possible because Posicor inhibits both CYP2D6 and CYP3A4.


Roche (Switzerland)


Different sources of media describe the Uses of 116666-63-8 differently. You can refer to the following data:
1. Vasodilator.
2. Mibefradil has been used as a T-type calcium channel blocker in various cells. It has also been used to reduce apoptosis of retinal ganglion cells (RGC) in EphB2-Fc.

Manufacturing Process

To the solution of 5.35 g (28 mmol) [3-(1H-benzimidazol-2- yl)propyl]methylamine in 12.5 mL toluene was added by syringe 12.5 mL (11.42 g, 114 mmol) isopropenyl acetate. The reaction mixture was heated to reflux temperature, and stirred at that temperature for 1.75 hours, with reaction completion monitored by thin-layer chromatography (silica gel, eluting with 70% ethyl acetate/30% methanol). The product, N-[3-(1Hbenzimidazol-2-yl)propyl]-N-methylacetamide, was obtained in quantitative yield.Under a dry nitrogen atmosphere, a 2.5 molar solution of butyl lithium in hexane, 8.4 mL (21 mmol) was added by syringe to 20 mL pentane. The solution was cooled to 0°C and 2.75 mL (2.13 g, 21 mmol) diisopropylamine was added by syringe over six min. The solution was warmed to 25°C and stirred for three hours, then volatiles were removed in vacuo. THF, 20 mL, was added via syringe to the residue, and the resulting yellow solution cooled to 0°C. A solution of 2.42 g (10.5 mmol) N-[3-(1H-benzimidazol-2-yl)propyl]- N-methylacetamide in 10 mL THF was added by syringe over 9 min. The yellow solution was stirred for 15 min, then cooled to -78°C. (S)-6-Fluoro-1- isopropyl-3,4-dihydro-1H-naphthalen-2-one, 2.166 g, 87.2% pure (97.6:2.4 S:R), in 2 mL toluene was added by syringe over 12 min, and a further 2 mL toluene was used to complete the transfer. After stirring for two hours, the viscous yellow mixture was added to 50 mL water at less than 10°C. The suspension that formed was extracted with diethyl ether; and the extracts were dried over anhydrous magnesium sulfate, filtered, and concentrated in vacuo to afford 3.74 g of impure (1S,2S)-N-[3-(1H-benzimidazol-2-yl)propyl]- 2-(6-fluoro-2-hydroxy-1-isopropyl-1,2,3,4-tetrahydronaphthalen-2-yl)-N-methylacetamide as a yellow foam. The foam was recrystallized from toluene, yield of a colorless solid 2.69 g, melting point 132-138°C. This material may be recrystallized a second time from toluene to remove residual (S)-6-fluoro- 1-isopropyl-3,4-dihydro-1H-naphthalen-2-one if necessary.(1S,2S)-N-[3-(1H-Benzimidazol-2-yl)propyl]-2-(6-fluoro-2-hydroxy-1- isopropyl-1,2,3,4-tetrahydronaphthalen-2-yl)-N-methylacetamidemay be synthesized by another method:To the mixture 22.7 g (0.54 mol) dry lithium chloride and 100 mL THF at - 15°C was added 160 mL 2 molar lithium diisopropylamide (0.32 mol) in heptane/THF/ethylbenzene was added. Then a solution of 36.6 g (0.16 mol) N-[3-(1H-benzimidazol-2-yl)-propyl]-N-methylacetamide in 140 mL toluene was added, the solution was stirred for 2 hours, and a further 155 mL toluene was added. (S)-6-Fluoro-1-isopropyl-3,4-dihydro-1H-naphthalen-2-one (29.9 g, 0.15 mol), in 15 mL toluene was added. After stirring at -10°C for 4 hours, the resulting solution was added to 200 mL ice water. The pH of the resulting mixture was adjusted to 7-8 by addition of a 71 g concentrated hydrochloric acid. The organic layer washed with water, then the solvents removed under reduced pressure to give 96 g of (1S,2S)-N-[3-(1H-benzimidazol-2-yl)propyl]- 2-(6-fluoro-2-hydroxy-1-isopropyl-1,2,3,4-tetrahydronaphthalen-2-yl)-Nmethylacetamide as a brown oil. The product was crystallysed from toluene, yield 45.3 g.(1S,2S)-N-[3-(1H-Benzimidazol-2-yl)propyl]-2-(6-fluoro-2-hydroxy-1- isopropyl-1,2,3,4-tetrahydronaphthalen-2-yl)-N-methylacetamide,20.22 g (45.7 mmol), dissolved in 200 mL toluene at 40°C, was added by cannula over 40 min at 0°C to a suspension of sodium bis(2-methoxyethoxy)aluminum hydride in toluene, 40 mL (41.44 g suspension, 26.94 g sodium bis(2- methoxyethoxy)aluminum hydride, 133 mmol). The mixture was stirred at 0°C for 15 min, then at 35-40°C for 3 hours. The mixture was cooled to 25°C then added carefully to 70 g sodium hydroxide in 140 g ice. The resulting suspension was warmed to 25°C over 30 min, and the phases were separated. The aqueous phase was extracted with toluene; and the organic phase was washed twice with 10% aqueous sodium hydroxide, once with water, then once with saturated brine. The toluene phase was dried and concentrated in vacuo to afford 20.61 g of (1S,2S)-2-[2-{[3-(1H-benzimidazol-2- yl)propyl]methylmethylamino}ethyl]-6-fluoro-1-isopropyl-1,2,3,4- tetrahydronaphthalen-2-ol as a colorless foam.To the mixture of 41.0 g (1S,2S)-2-[2-{[3-(1H-benzimidazol-2- yl)propyl]methylmethylamino}ethyl]-6-fluoro-1-isopropyl-1,2,3,4- tetrahydronaphthalen-2-ol, 240 mL water, and 240 mL toluene were added 22.4 g potassium hydroxide, and the mixture heated to 45-50°C for one hour. The resulting two-phase mixture was separated. To the organic phase was added 39.4 g (4.0 eq.) potassium carbonate sesquihydrate; then a solution of 21.0 g (17.7 mL, 3.25 eq.) methoxyacetyl chloride in 33 mL toluene was added over two hours at 25-30°C, and the resulting mixture stirred for an additional 30 min. Water, 200 mL, was added to quench the reaction. The organic phase, containing mibefradil as the free base was added an ethanol. To the stirred mixture of mibefradil and ethanol was added at 20°C a solution of 4.4 g of hydrogen chloride in 44.6 mL (35.0 g) ethanol. The mixture was heated to 50°C and 1.0 mL water was added, followed by a solution of 3.4 mL water in 332 mL methyl tert-butyl ether over one hour. The mixture was stirred for 3 hours. Mibefradil dihydrochloride crystals was seeded. A solution of 0.6 mL water in 65 mL methyl tert-butyl ether was added over one hour, and the mixture aged for a further 1.5 hours. The mixture was then cooled, and the resulting slurry of mibefradil dihydrochloride was filtered; yield 95%.

Brand name

Posicor (Hoffmann-LaRoche).

Therapeutic Function

Coronary vasodilator

Biochem/physiol Actions

Mibefradil is a tetralol derivative and nondihydropyridine calcium channel blocker. It blocks long-type (L-type) calcium channels. It blocks mildly the Purkinje-type (P-type) calcium channels in Purkinje neurons.

Check Digit Verification of cas no

The CAS Registry Mumber 116666-63-8 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,1,6,6,6 and 6 respectively; the second part has 2 digits, 6 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 116666-63:
138 % 10 = 8
So 116666-63-8 is a valid CAS Registry Number.

116666-63-8 Well-known Company Product Price

Brand (Code)Product description CAS number Packaging Price Detail
Sigma (M5441)  Mibefradil dihydrochloride hydrate  ≥98% (HPLC), powder 116666-63-8 M5441-5MG 1,419.21CNY Detail
Sigma (M5441)  Mibefradil dihydrochloride hydrate  ≥98% (HPLC), powder 116666-63-8 M5441-25MG 4,923.36CNY Detail



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

Version: 1.0

Creation Date: Aug 13, 2017

Revision Date: Aug 13, 2017


1.1 GHS Product identifier

Product name Mibefradil dihydrochloride hydrate

1.2 Other means of identification

Product number -
Other names [(1S,2S)-2-[2-[3-(1H-benzimidazol-2-yl)propyl-methylamino]ethyl]-6-fluoro-1-propan-2-yl-3,4-dihydro-1H-naphthalen-2-yl] 2-methoxyacetate,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:116666-63-8 SDS

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