β Scribed by Chun-Won Jung; Liu-Lan Shen; Brian Hyun Choi; Young-Shin Kwak; Jin-Hyun Jeong
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A library of 2,3-disubstituted benzofuran scaffold was developed by using intramolecular Wittig olefination and Friedel-Crafts acylation.
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3-Iodobenzoic acid was loaded on Rink amide resin. Pd(0) coupling reaction with tributyl(1-ethoxyvinyl)tin followed by bromination using NBS gave an a-bromoketone bound to a solid support. Condensation of thioamide or thiourea, followed by TFA cleavage from the resin, gave 2,4-disubstituted thiazole
A versatile method for the solid phase synthesis of oxazolidin-2-ones is described. A resin bound phenolic group was treated with (Β±)-epichlorohydrin followed by opening of the epoxide ring with sodium azide. The resulting 1-azido-3-aryloxypropan-2-ol was treated with p-nitrophenylchloroformate and
An efficient method for the traceless solid phase synthesis of 2,3-disubstituted indoles using a THP linker and a Pd(0)-mediated annulation of 2-iodoaniline and acetylenes is reported.