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Efficient Chemo-Enzymatic Flow Synthesis of High Value Amides and Esters
| Content Provider | MDPI |
|---|---|
| Author | Annunziata, Francesca Contente, Martina Letizia Betti, Daniele Pinna, Cecilia Molinari, Francesco Tamborini, Lucia Pinto, Andrea |
| Copyright Year | 2020 |
| Description | 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–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. |
| Starting Page | 939 |
| e-ISSN | 20734344 |
| DOI | 10.3390/catal10080939 |
| Journal | Catalysts |
| Issue Number | 8 |
| Volume Number | 10 |
| Language | English |
| Publisher | MDPI |
| Publisher Date | 2020-08-16 |
| Access Restriction | Open |
| Subject Keyword | Catalysts Organic Chemistry Flow Chemistry Biocatalysis Immobilisation Active Pharmaceutical Ingredients Flow Hydrogenation |
| Content Type | Text |
| Resource Type | Article |
