[reaction: see text] A general strategy toward macrocyclic compounds using multicomponent reaction (MCR) chemistry, e.g., Passerini and Ugi variants, and ring-closing metathesis (RCM) is introduced. The corresponding bifunctional isocyanides carboxylic acids bearing a terminal olefin are easy to prepare from the corresponding commercially available starting materials. Advantageously, this strategy allows fast access to a diverse conformational space of natural product-like macrocycles and could thus be of interest in the discovery of novel bioactive agents.

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Short and Diverse Route Toward Complex Natural Product-Like Macrocycles. -Carboxylic acid (III), obtained from biphenylcarboxylic acid anhydride (I) undergoes Passerini reaction with paraformaldehyde and isocyanide (VI) to form (VIII). Subsequent ring-closing metathesis reaction using Grubb's catalyst results in the formation of macrocycle (IX). The present new procedure including a multicomponent reaction and ring-closing metathesis demonstrates a short and diverse route toward complex natural macrocycles. -(BECK, B.; LARBIG, G.; MEJAT, B.; MAGNIN-LACHAUX, M.; PICARD, A.; HERDTWECK, E.; DOEMLING*, A.; Org. Lett. 5 (2003) 7,

Thiazole derivatives Thiazole derivatives R 0260 Convergent Multicomponent Assembly of 2-Acyloxymethyl Thiazoles. -A novel three-component reaction of acrylate (I), thiocarboxylic acids and aldehydes is described. However, the yields of the biologically interesting 2-acyloxymethyl thiazoles (IV) are only low to moderate. -(HENKEL, B.; BECK, B.; WESTNER, B.; MEJAT, B.; DOEMLING*, A.; Tetrahedron Lett. 44 (2003) 50, 8947-8950;