105878-43-1

Basic information

• Product Name: bisoprolol Fumarate
• Synonyms: bisoprolol Fumarate
• CAS NO: 105878-43-1
• Molecular Weight: 441.522
• Mol File: 105878-43-1.mol
• Article Data: 5

Chemical Properties

• CAS DataBase Reference: bisoprolol Fumarate(CAS DataBase Reference)
• NIST Chemistry Reference: bisoprolol Fumarate(105878-43-1)
• EPA Substance Registry System: bisoprolol Fumarate(105878-43-1)

Safety Data

• Hazardous Substances Data: 105878-43-1(Hazardous Substances Data)

Upstream product

• 111051-40-2 bisoprolol 
• 110-17-8 (2E)-but-2-enedioic acid 
• 66722-65-4 N-[2-hydroxy-3-(p-2-isopropoxyethoxymethylphenoxy)-propyl]-N-isopropyl-acetamide 
• 66722-64-3 1-(p-2-isopropoxyethoxymethylphenoxy)-3-isopropylideneamino-propan-2-ol 
• 66722-57-4 2-((4-((2-isopropoxyethoxy)methyl)phenoxy)methyl)oxirane 

Downstream Products

• 111051-40-2 bisoprolol 
• 109-59-1 2-(1-methylethoxy)-ethanol 

Relevant articles and documents

Polymorphic forms of bisoprolol fumarate: Preparation and characterization

Bisoprolol fumarate is a beta blocker-type drug substance which has been well known for several decades. However, no relevant data can be found in the literature about its crystal polymorphism. The purpose of this paper was to present two anhydrous forms (Form I and Form II) and a hydrate of bisoprolol fumarate substance. Crystalline forms were studied by various solid-state analytical methods: Fourier transform infrared (FT-IR) spectroscopy, X-ray powder diffraction (XRPD), dynamic vapor sorption (DVS) and thermoanalytical methods (thermogravimetry and differential scanning calorimetry). Thermodynamic stability and solubility of the presented polymorphs were also investigated. Both FT-IR and XRPD methods were found to be suitable for the characterization of the different crystal structures. Thermoanalytical measurements showed that (1) Form I and Form II own clearly different melting points and (2) both Form II and hydrate forms can transform into Form I at higher temperature values. Results of the DVS measurements prove that both Form I and Form II became metastable under extremely humid conditions (> 80% RH) and converted into the hydrate. Thermodynamic stability studies showed that Form I and Form II polymorphs are in enantiotropic relationship with an enantiotropic point at about 40–45?°C. Solubility studies indicated that all of the prepared forms are highly soluble, and no difference was found between them. Considering the recommendations of the corresponding International Conference of Harmonization guideline, it can be stated that no specification is required for crystal polymorphism in case of this substance.

A NOVEL PROCESS FOR THE SYNTHESIS OF BISODPROLOL AND ITS INTERMEDIATE

This invention relates to a manufacturing process for the preparation of bisoprolol and its pharmaceutically acceptable salt as well as its intermediates. The intermediate 4-[(2-isopropoxyethoxy)methyl]phenol is prepared by reaction of 4-hydroxybenzyl alcohol with 2-isopropoxy ethanol in presence of Amberlyst 15 in high yield with high purity.

PHENOXY- AMINO-PROPANOLS

New phenoxy-amino-propanols of formula STR1 wherein R 1 is alkenyl, alkynyl, alkoxyalkyl or alkenyloxyalkyl with 2-6 C atoms in each case or cycloalkyl with 3-8 C atoms; and R 2 is alkyl or hydroxyalkyl with 1-6 C atoms in each case, cycloalkyl with 3-8 C atoms, aralkyl or aralkyl wherein the aryl radical is mono-to tri-substituted by alkyl, alkoxy, OH, F and/or Cl or mono-substituted by methylenedioxy, with a total of 7-15 C atoms in each case, and the physiologically acceptable acid addition salts thereof, exhibit various pharmacological properties including isoprenaline-antagonism on the heart rate and blood pressure.