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Ars Pharmaceutica (Internet)

On-line version ISSN 2340-9894


CORNIER, Patricia Griselda. Scale-up synthesis of TAP7f, an antitumoral triazolyl peptidyl penicillin. Ars Pharm [online]. 2020, vol.61, n.3, pp.169-173.  Epub Aug 17, 2020. ISSN 2340-9894.


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.


Solution chemistry strategies were used to replace the original synthetic solid phase route to make the process more profitable.


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.


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.

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