ONE-POT SYNTHESIS OF 4,5-DIHYDRO-3,1-BENZOXAZEPINE-2(1H)-THIONES FROM 2-(2-ISOCYANOPHENYL)ETHANOLS VIA THE CORRESPONDING ISOTHIOCYANATES

[摘要]：An efficient method for the preparation of 4,5-dihydro-3,1-benzoxazepine-2(1H)-thiones under mild conditions has been developed. 2-(2-Isocyanophenyl)ethanols, easily accessible by treating 1-isocyano-2-(lithiomethyl)benzenes with aldehydes or ketones, were converted into the corresponding isothiocyanates on treatment with sulfur in the presence of a catalytic amount of selenium and excess triethylamine. These isothiocyanato alcohols were then treated with sodium hydride to give 4,5-dihydro-3,1-benzoxazepine-2(1H)-thione derivatives in one pot.

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