N-Acylsulfonamide safety-catch linkers are versatile tools in solid-phase organic synthesis because of their stability. This stability necessitates linker activation prior to compound cleavage. Here, we demonstrate that the N-acylsulfonamide group can react with a pi-allyl palladium complex and that these mild and neutral conditions can be exploited for linker activation. The advantages of this...

Novel, efficient and mild preparation of 7- and 8-membered cyclic di- and 10-membered cyclic tripeptides containing α-, β- or γ-amino acid residues is effected by a Staudinger-mediated ring closure. Medium-sized cyclic di- and tripeptides--recognized as difficult targets--were obtained in moderate to good yields according to a straightforward sequence. Empirical force-field calculations were un...

Krystyna Lesiak and Wojciech J. Stec Polish Academy of Sciences, Centre of Molecular and Macromolecular Studies, 90-362 Lodz, Boczna 5, Poland Z. Naturforsch. 33b, 782-785 (1978); received March 28, 1978 1,3,2-Oxazaphospholidines, (—)Ephedrine, Thioanilides, Thioesters, Stereochemistry Both isomers of 2-anilido-3,4-dimethyl-5-phenyl-l,3,2-oxazaphospholidine-2-thiones (2 a and 2 b) derived from ...