Scale-up synthesis of TAP7f, an antitumoral triazolyl peptidyl penicillin

Abstract

Abstract Purpose: The purpose of this work was to develop a synthetic process to obtain the compound with anti-tumor activity, TAP7f, on a gram scale, for preclinical studies. Method: Solution chemistry strategies were used to replace the original synthetic solid phase route to make the process more profitable. Results: TAP7f was obtained from an inexpensive starting material L-phe, in five-steps and using less amounts of reagents, rendering this new process more amenable to the large-scale production. Conclusions: We have demonstrated that this new, procedure is a more efficient and economical route to synthesize the target molecule in large scale.

Keywords

• antitumoral
• scale-up
• Triazolyl peptidyl penicillins