Enzyme cascades represent an important technology to develop environmentally friendly and cheap synthetic processes to obtain drugs1 by combining different transformations in sequential reactions. In this context, the joint combination of both biocatalysts and green solvents as environmentally responsible reaction media and catalysts is seen by many as an important strategy towards this goal, with an improvement of (enantio)selectivity and a concomitant reduction of potential hazards.2 In this communication, we report on two sequential transformations carried out in unconventional media, which are based on a kinetic resolution of racemic secondary alcohols followed by a carbon-carbon Negishi cross-coupling reaction3 en route to some pharmaceutically relevant drugs with anti-Alzheimer activity (Scheme 1).4
Multistep Enzyme Cascades and Metal-catalyzed Reactions in Unconventional Media for the Synthesis of Pharmaceutically Relevant Molecules
Mara Pulpito;Giuseppe Dilauro;Luciana Cicco;Paola Vitale;Filippo M. Perna;Antonino Biundo;Vito Capriati
2022-01-01
Abstract
Enzyme cascades represent an important technology to develop environmentally friendly and cheap synthetic processes to obtain drugs1 by combining different transformations in sequential reactions. In this context, the joint combination of both biocatalysts and green solvents as environmentally responsible reaction media and catalysts is seen by many as an important strategy towards this goal, with an improvement of (enantio)selectivity and a concomitant reduction of potential hazards.2 In this communication, we report on two sequential transformations carried out in unconventional media, which are based on a kinetic resolution of racemic secondary alcohols followed by a carbon-carbon Negishi cross-coupling reaction3 en route to some pharmaceutically relevant drugs with anti-Alzheimer activity (Scheme 1).4I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.