Abstract
The enzymatic method was used for the direct biotransformation of racemic atenolol. The catalytic activities of commercially available lipases from Candida rugosa were tested for the kinetic resolution of (R,S)-atenolol by enantioselective acetylation in various two-phase reaction media containing ionic liquids. The composed catalytic system gave the possibility to easy separate substrates and products of the conducted enantioselective reaction and after specific procedure to reuse utilized enzymes in another catalytic cycle.
Highlights
The growing demand of optically pure compounds for pharmaceutical, chemical, and cosmetic industries is fully understood by scientists, which is confirmed by the increasing number of papers published in this area. β-blockers are one of the classes of drugs, which are playing a relevant role in the treatment of various human diseases
The enantioselective biotransformation of (R,S)-atenolol was investigated with the use of commercially available lipase from Candida rugosa OF and MY (Figure 1) in various two-phase reaction media
The two-phase catalytic systems composed by ionic liquid and toluene, as well as lipase from Candida rugosa, and acetylating agent allowed to obtain high enantioselective parameters
Summary
The growing demand of optically pure compounds for pharmaceutical, chemical, and cosmetic industries is fully understood by scientists, which is confirmed by the increasing number of papers published in this area. β-blockers are one of the classes of drugs, which are playing a relevant role in the treatment of various human diseases. Atenolol is included to the compounds of an amino-alcohols and is frequently used in treatment of hypertension, angina pectoris, and arrythmia [1–5]. All β-blockers possess chiral carbon atom within their moiety, they are presented as enantiomers. It was described in many research studies, that the (S)-enantiomers of abovementioned APIs are responsible for the desired therapeutic effects, β-blockers are still widely commercially available and administrated to patients as racemates. The replacement of racemic drugs into optically pure compounds would cause less side effects. In order to achieve this effect, there are many various strategies as well as chemical synthesis, which allow to obtain enantiomerically pure compounds, including (S)-enantiomers of β-blockers [6–9]
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
