Selection of the Parameters in the Synthesis of Ethylenediamine-Folate Using the Plackett Burman Design

Autor: Erianti Siska Purnamasari, Linda Septiana, Ari Hardianto, Ukun Mochammad Syukur Soedjanaatmadja, Anni Anggraeni, Husein Hernadi Bahti
Jazyk: angličtina
Rok vydání: 2022
Předmět:
Zdroj: Indonesian Journal of Chemistry, Vol 22, Iss 3, Pp 599-608 (2022)
Druh dokumentu: article
ISSN: 1411-9420
2460-1578
DOI: 10.22146/ijc.68313
Popis: This study is concerned with synthesizing ethylenediamine-folate (EDA-Folate), which will then be used as a precursor in synthesizing Gd-PEG-DOTA-Folate, a novel targeted-contrast agent for the diagnosis of cancer, employing the Magnetic Resonance Imaging method. This study aims to determine all the parameters affecting the synthesis of EDA-Folate using the Plackett Burman design. The synthesis method included activation of folic acid using dicyclohexylcarbodiimide and N-Hydroxysuccinimide to result in NHS-Folate, followed by conjugation of ethylenediamine with NHS-Folate to produce EDA-Folate. Analysis of the reaction product confirmed that the reaction product was EDA-Folate. From the resulted data, it can also be concluded that there were four significant parameters (out of the ten parameters studied) in the synthesis of EDA-Folate (with its value presented in the bracket), i.e., time inactivation of NHS-Folate (24 h), stirring rate inactivation of NHS-Folate (300 rpm), the mole of EDA (12 moles), and time of EDA-Folate (12 h). Moreover, the value or desirability of the experimental design was found to be 0.875 (which is < 1.0), meaning that the design will produce optimal conditions and thus the optimal yield of the reaction.
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