Efficient Chemo-Enzymatic Flow Synthesis of High Value Amides and Esters
| Autor: | Lucia Tamborini, Daniele Betti, Francesca Annunziata, Andrea Pinto, Martina Letizia Contente, Francesco Molinari, Cecilia Pinna |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2020 |
| Předmět: |
active pharmaceutical ingredients
biocatalysis flow chemistry Chemo enzymatic 010402 general chemistry lcsh:Chemical technology 01 natural sciences Chloride Catalysis lcsh:Chemistry chemistry.chemical_compound Amide Bioreactor medicine lcsh:TP1-1185 Physical and Theoretical Chemistry Reusability biology 010405 organic chemistry Mycobacterium smegmatis Butacaine biology.organism_classification Combinatorial chemistry 0104 chemical sciences immobilisation chemistry lcsh:QD1-999 Acyltransferase flow hydrogenation medicine.drug |
| Zdroj: | Catalysts, Vol 10, Iss 939, p 939 (2020) Catalysts Volume 10 Issue 8 |
| ISSN: | 2073-4344 |
| Popis: | A flow-based chemo-enzymatic synthesis of selected APIs (i.e., butacaine, procaine and procainamide) has been developed. A bioreactor made of MsAcT, a versatile acyltransferase from Mycobacterium smegmatis, immobilised on glyoxyl&ndash garose, was exploited to efficiently prepare amide and ester intermediates in gram scale. Immobilised MsAcT was employed in pure organic solvent, demonstrating high stability and reusability. In-line purification of the key intermediates using polymer-bound sulphonyl chloride was added after the bioreactor, enhancing the automation of the process. A final hydrogenation step using the H-Cube reactor was further carried out to obtain the selected APIs in excellent yields (> 99%), making the process fast, safe and easily handled. |
| Databáze: | OpenAIRE |
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