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Ars Pharmaceutica (Internet)
On-line version ISSN 2340-9894
Abstract
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. https://dx.doi.org/10.30827/ars.v61i3.15210.
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.