208523-18-6Relevant articles and documents
Preparation method of chiral bisoprolol fumarate
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Paragraph 0052-0057, (2021/01/20)
The invention provides a preparation method of chiral bisoprolol fumarate. The preparation method comprises the following steps: preparation of (S)-bisoprolol fumarate and preparation of (R)-bisoprolol fumarate. According to the preparation method of the chiral bisoprolol fumarate, provided by the invention, isopropoxyethoxymethylphenol and sulfonyl chloride are subjected to esterification reaction to generate a sulfonate compound, the compound reacts with chiral epoxypropanol to generate a chiral epoxy compound, the compound is subjected to a ring-opening reaction to obtain chiral bisoprolol,and the chiral bisoprolol is subjected to a salt forming reaction to obtain chiral bisoprolol fumarate, wherein the obtained product is high in single configuration purity, so that the method has themain advantages that the raw materials are easy to obtain, the process is simple, economical and environment-friendly, and industrial production is facilitated.
Polymorphic forms of bisoprolol fumarate: Preparation and characterization
Detrich, ádám,D?m?t?r, Kata Judit,Katona, Miklós Tamás,Markovits, Imre,Vargáné Láng, Judit
, (2018/07/30)
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.
MANUFACTURE OF BISOPROLOL AND INTERMEDIATES THEREFOR
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Page/Page column 12-13, (2010/06/17)
A process for preparing bisoprolol comprises reacting oxazolidinone sulphonate with 4-hydroxybenzylaldehyde to form oxazolidinone benzaldehyde, forming oxazolidone benzylalcohol from oxazolidone benzaldehyde, and subsequently reacting oxazolidinone benzylalcohol with isopropyl oxitol to form bisoprolol base. Oxazolidone sulphonate and oxazolidone benzaldehyde are novel intermediates.
A NOVEL PROCESS FOR THE SYNTHESIS OF BISODPROLOL AND ITS INTERMEDIATE
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Page/Page column 5; 9-10, (2010/11/27)
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.
CsF in organic synthesis. The first and convenient synthesis of enantiopure bisoprolol by use of glycidyl nosylate
Kitaori, Kazuhiro,Furukawa, Yoshiro,Yoshimoto, Hiroshi,Otera, Junzo
, p. 3173 - 3176 (2007/10/03)
The regioselective substitution of glycidyl nosylate with phenols is catalyzed by CsF in the presence of K2CO3 in DMF; this reaction enables the first and convenient synthesis of enantiopure bisoprolol.
Controlled release pharmaceutical preparation
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, (2008/06/13)
A controlled release pharmaceutical preparation comprising a core containing a medicinal compound and a coating layer containing a water-repellent salt and a water-insoluble and slightly water-permeable acrylic polymer having trimethylammoniumethyl group. Said preparation releases a medicinal compound in a sigmoid type dissolution pattern irrespective of the PH of a dissolution medium.
PHENOXY- AMINO-PROPANOLS
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, (2008/06/13)
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.
