MIBEFRADIL

Base Information

• Chemical Name: MIBEFRADIL
• CAS No.: 116666-63-8
• Molecular Formula: C29H38 F N3 O3 . 2 Cl H
• Molecular Weight: 568.55
• Mol file: 116666-63-8.mol

Synonyms:Aceticacid, 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, dihydrochloride (9CI); Acetic acid, methoxy-, 2-[2-[[3-(1H-benzimidazol-2-yl)propyl]methylamino]ethyl]-6-fluoro-1,2,3,4-tetrahydro-1-(1-methylethyl)-2-naphthalenylester, dihydrochloride, (1S-cis)-; Mibefradil dihydrochloride; Posicor; Ro40-5967; Ro 40-5967/001

Chemical Property of MIBEFRADIL

Chemical Property:

• Vapor Pressure: 1.17E-16mmHg at 25°C
• Melting Point: 128℃
• Boiling Point: 647.6°Cat760mmHg
• PKA: 4.8; 5.5(at 25℃)
• Flash Point: 345.5°C
• PSA: 67.45000
• Density: g/cm³
• LogP: 6.87490
• Storage Temp.: under inert gas (nitrogen or Argon) at 2-8°C
• Solubility.: H2O: 24 mg/mL, soluble

Purity/Quality:

97% ^*data from raw suppliers

MibefradilDihydrochloride ^*data from reagent suppliers

Safty Information:

• Pictogram(s):  
• Hazard Codes: 

MSDS Files:

SDS file from LookChem

Total 1 MSDS from other Authors

Useful:

• Description: 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.
• Uses: Vasodilator. 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.
• Therapeutic Function: Coronary vasodilator

Technology Process of MIBEFRADIL

There total 4 articles about MIBEFRADIL which guide to synthetic route it. The literature collected by LookChem mainly comes from the sharing of users and the free literature resources found by Internet computing technology. We keep the original model of the professional version of literature to make it easier and faster for users to retrieve and use. At the same time, we analyze and calculate the most feasible synthesis route with the highest yield for your reference as below:

synthetic route:

Reference yield:

→ mibefradil (116666-63-8,116644-53-2)

Guidance literature:

Reference yield:

→ mibefradil (116666-63-8,116644-53-2) + mibefradil dihydrochloride (116666-63-8)

Guidance literature:

Reference yield:

→ mibefradil (116666-63-8,116644-53-2) + mibefradil dihydrochloride (116666-63-8)

Guidance literature:

upstream raw materials:

Methoxyacetyl chloride

(1S,2S)-2-[2-{[3-(1H-benzimidazol-2-yl)propyl]methylamino}ethyl]-6-fluoro-1-isopropyl-1,2,3,4-tetrahydronaphthalen-2-ol