No abstract

TBAF-assisted N-arylation and benzylation of benzazoles such as 1H-benzimidazole, 1H-indole, and 1H-benzotriazole with aryl and benzyl halides have been demonstrated under the ligand/base/solvent-free conditions. In the presence of CuBr2 and TBAF (n-Bu4NF), the azoles underwent N-arylation and benzylation with aryl and benzyl halides smoothly in moderate to good yields. It is noteworthy that the reaction is conducted under the ligand/base/solvent-free conditions.

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(4,5-Dichloro-6-oxo-6H-pyridazin-1-yl)phosphoric acid diethyl ester (3a) are efficient and selective coupling agents for the amidation of carboxylic acids. Amidation of aliphatic and aromatic carboxylic acids with aliphatic and aromatic amines using 3a under mild condition gave chemoselectively the corresponding amides in good to excellent yield. Three protected-dipeptides were also synthesized from N-BOC-Phe and O-Meamino acid hydrochlorides using 3a under mild condition.

(4,5-Dichloro-6-oxo-6H-pyridazin-1-yl)phosphoric acid diethyl ester (3) is an efficient coupling agent for lactonization of aliphatic and aromatic ω-hydroxycarboxylic acids. Lactonization of ω-hydroxycarboxylic acids with 3 in the presence of equimolar amounts of a base gave the corresponding monoolides, diolides, triolides and/or tetraolides.