Preparation of 2-Heteroaryl-indolin-3-ones by Acid-Mediated Intramolecular Cyclization in Batch and Flow.

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Tác giả: Yiding Chen, Shuyu Liu, Matthew G Lloyd, Loïc R E Pantaine, Zeynep Saglam, Aaron J Senior

Ngôn ngữ: eng

Ký hiệu phân loại: 025.342 *Clippings, broadsides, pamphlets

Thông tin xuất bản: United States : Organic letters , 2025

Mô tả vật lý:

Bộ sưu tập: NCBI

ID: 198082

An intramolecular cyclization strategy to synthesize nitrogen-rich and biologically important 2-heteroaryl-indolin-3-ones has been developed in both batch and flow. Using high-throughput screening, citric acid in a dimethylformamide/water mixture was found to facilitate the reaction under batch conditions, which can tolerate substituted phenyl rings, quinolines, and naphthalenes with a variety of electronic and steric properties. The reaction was reoptimized for flow conditions using design of experiments, complementing the batch conditions for some substrates with greatly reduced reaction times.
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