Abstract
| - The solid-phase synthesis of 1,5-disubstituted2-aryliminoimidazolidines, starting from resin-bound N-acylated amino acid amides, is described. Exhaustive reduction of resin-bound acylated amino acid amides with borane−THF afforded the corresponding disecondary amines. Furtherreaction with arylisothiocyanates in the presence of mercuricchloride (HgCl2) yielded the corresponding resin-bound 1,5-disubstituted 2-aryliminoimidazolidines. Cleavage of theproduct from the resin using HF/anisole (95/5) for 1.5 h at 0°C gave the desired products in good yield and purity. Thepreparation of a large combinatorial library of such compounds is also discussed.
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