Process development of a dual MMP/TNF inhibitor (SDZ 242-484)

…, G Kottirsch, B Wietfeld, E Küsters

Index: Koch, Guido; Kottirsch, Georg; Wietfeld, Bernhard; Kuesters, Ernst Organic Process Research and Development, 2002 , vol. 6, # 5 p. 652 - 659

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Citation Number: 23

Abstract

The compound (2 R, 3 S)-N-4-((S)-2, 2-Dimethyl-1-methylcarbamoyl-propyl)-N-1-hydroxy-2- hydroxymethyl-3-(4-methoxy-phenyl) succinamide (1; SDZ 242-484) shows antiinflammatory effects due to inhibition of matrix metalloproteases (MMP) and tumor necrosis factor-α activity (TNF). We describe the development of a chromatography-free process for a multikilogram-scale pilot-plant production. Two of the three chiral centers are introduced in ...