脂环族 β-和 γ-氨基酸：用于立体控制构建基于氨基酸的碳环核苷类似物的有用骨架。
Alicyclic β- and γ-Amino Acids: Useful Scaffolds for the Stereocontrolled Access to Amino Acid-Based Carbocyclic Nucleoside Analogs.
机构信息
Institute of Pharmaceutical Chemistry, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary.
Interdisciplinary Excellence Centre, Institute of Pharmaceutical Chemistry, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary.
出版信息
Molecules. 2019 Jan 3;24(1):161. doi: 10.3390/molecules24010161.
Stereocontrolled synthesis of some amino acid-based carbocyclic nucleoside analogs containing ring C=C bond has been performed on β- and γ-lactam basis. Key steps were -arylation of readily available β- or γ-lactam-derived amino ester isomers and amino alcohols with 5-amino-4,6-dichloropyrimidine; ring closure of the formed adduct with HC(OMe)₃ and nucleophilic displacement of chlorine with various -nucleophiles in the resulting 6-chloropurine moiety.
已在β-和γ-内酰胺的基础上进行了一些含有环 C=C 键的基于氨基酸的碳环核苷类似物的立体控制合成。关键步骤是：用 5-氨基-4,6-二氯嘧啶与易得的β-或γ-内酰胺衍生的氨基酸酯异构体和氨基酸醇进行 -芳基化；用 HC(OMe)₃ 闭环形成的加合物，并在所得的 6-氯嘌呤部分用各种 -亲核试剂进行氯的亲核取代。
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