A green and efficient synthesis of benzo[d][1,3]thiazines through a base-promoted cyclization reaction of o-isothiocyanato arylacetylenes with aroylacetonitriles has been developed. This protocol features high step economy and efficiency, and tolerates various functional groups. The reaction was scalable and applied for the post-modification of drugs.
Jian Shen, Shumin Li, Zhenyu Yao, Shenghui Lin, Xiuling Cui. Base-promoted cyclization reaction of o-isothiocyanato arylacetylenes and aroylacetonitriles: easy access to benzo[d][1,3]thiazines. Organic & biomolecular chemistry. 2022 Sep 21;20(36):7236-7240
PMID: 36069145
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