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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.  http://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.

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