Solid-phase synthesis of 1,5-disubstituted 2-aryliminoimidazolidines |
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Authors: | Yu Yongping Ostresh John M Houghten Richard A |
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Institution: | Torrey Pines Institute for Molecular Studies, 3550 General Atomics Court, San Diego, California 92121, USA. |
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Abstract: | The solid-phase synthesis of 1,5-disubstituted 2-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. Further reaction with arylisothiocyanates in the presence of mercuric chloride (HgCl(2)) yielded the corresponding resin-bound 1,5-disubstituted 2-aryliminoimidazolidines. Cleavage of the product from the resin using HF/anisole (95/5) for 1.5 h at 0 degrees C gave the desired products in good yield and purity. The preparation of a large combinatorial library of such compounds is also discussed. |
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