Tong Jinghui, Guo Shilin, Zhu Huajie, Ouyang Lu, Liao Jianhua, Li Youchun
School of Pharmacy, Gannan Medical University Ganzhou 341000 Jiangxi Province P. R. China
The Affiliated Ganzhou Hospital, Jiangxi Medical College, Nanchang University Ganzhou 341000 Jiangxi Province P. R. China.
RSC Adv. 2024 Nov 29;14(51):38105-38109. doi: 10.1039/d4ra07386j. eCollection 2024 Nov 25.
β- and γ-Amino alcohols are among the most significant structural motifs in pharmacologically active molecules and pharmaceuticals. Herein, a protocol for the construction of β- and γ-amino alcohols reductive amination and transfer hydrogenation of diketones with aromatic amines is described. This reaction is performed by utilizing iridium complexes as catalysts and HCOH as a hydrogen donor to deliver a library of β- and γ-amino alcohols under mild and operationally simple conditions. Successful scale-up performance was also conducted under standard conditions.
β-和γ-氨基醇是药理活性分子和药物中最重要的结构基序之一。本文描述了一种通过二酮与芳香胺的还原胺化和转移氢化反应构建β-和γ-氨基醇的方法。该反应以铱配合物为催化剂,以HCOH为氢供体,在温和且操作简单的条件下生成一系列β-和γ-氨基醇。在标准条件下还成功进行了放大反应。