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Optimization of AR-3 synthesis

Andrzej Leś 1,2Katarzyna Badowska-Rosłonek 1Marta Łaszcz 1Agata E. Kamieńska-Duda 1Piotr Baran 1Łukasz S. Kaczmarek 1

1. Pharmaceutical Research Institute (IF), Rydygiera 8, Warszawa 01-793, Poland
2. Warsaw University, Faculty of Chemistry, Pasteura 1, Warszawa 02-093, Poland


The reaction of quinolinone derivative 1 with piperazine derivative 2 giving AR-3 was carried out at laboratory scale (10 mmol of 1 ) under various conditions in order to achieve high yield and purity of the product. The reaction parameters (1 : 2 ratio, amount of base, volume of ethanol and the reaction timing) were sampled guided by the D-optimal plans. Molar content of crude reaction product was predicted theoretically with the use of the mass balance and the corresponding HPLC parameters. The theoretical predictions were verified with the potentiometric and thermogravimetric analysis for selected samples. Based on the predicted molar content of reaction mixtures a series of reaction response surfaces was calculated. From analysis of these surfaces it appears that there exists an optimal set of reaction parameters for AR-3 synthesis for a high conversion ratio of about 99 % and 99.5 % purity of the product.

Keywords: optimization, synthesis, reaction response surface







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Submitted: 2008-03-10 15:08
Revised:   2009-06-07 00:48