Studies On The Synthetic Process Of Darbufelone And Its Me-too Compounds

On the basis of non-steroidal anti-inflammatory drug( NSAIDs). we have done a research in synthetic technic of Darbufelone. Darbufelone is a new dual inhibitors of COX-2 and LOX-5. In this paper, Darbufelone mesilate was synthesized. Emphases were laid on the synthetic technology of 3,5-ditertbutyl-4-hydroxybenzaldehyde and 2-aminothiazolidin-4-one. The condensation reaction of 3,5-ditertbutyl-4-hydroxybenzaldehyde and 2-aminothiazolidin-4-one was also explored.An industrial synthetic route was achieved. At the same time, we have done primary pharmacological research in anti-inflammatory activities of Darbufel-olone. The experimental result indicated that Darbufelone has favourable anti-inflammatory effect. Other pharmacological tests of Darbufelone are being carried out.According to drug metabolism theory in vivo and the idea of prodrug design,three new Me-too compounds of Darbufelone were designed and synthesized. Other pharmacological tests are being carried out.