A highly efficient flow reactor process for the synthesis of N-Boc-3,4-dehydro-l-proline methyl ester

    • Lucia Tamborini
    • Paola Conti
    • Andrea Pinto
    • Carlo De Micheli
    • Dipartimento di Scienze Farmaceutiche ‘Pietro Pratesi’,
    • Università degli Studi di Milano, Italy

    The multi-step preparation of N-Boc-3,4-dehydro-l-proline methyl ester using a modular flow reactor is reported. The use of immobilised reagents and scavengers in pre-packed glass tubes allows us to obtain the pure product in 87% overall yield, 97% purity, and >98% enantiomeric excess without any additional purification step. Our flow-based protocol enables the rapid multi-gram synthesis (about 9 g/12 h) of the desired product.

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