Describes a scalable, 60%-yield chemoenzymatic synthesis method for doxorubicin-14-O-esters that avoids chromatographic purification.
May enable doxorubicin-ester research access; leaves clinical translation open pending validation.
An efficient three-step, chemoenzymatic synthesis of unprotected doxorubicin-14-O-esters from doxorubicin hydrochloride salt is described. The key step is a lipase-catalyzed regioselective transesterification/esterification using commercially available acyl donors and doxorubicin reversibly derivatized with N-alloc to improve substrate loadings. The overall yield is ca. 60% and chromatographic purification is not required, thereby making the process more amenable to scale-up.
No takes yet. Share an insight, caveat, or question.
Cotterill et al. (2008) studied this question.
Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context: