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Synthesis of Bridged Bicyclic Morpholine Amino Acids as Compact Modules for Medicinal Chemistry
Chemistry Letters ( IF 1.4 ) Pub Date : 2017-04-05 , DOI: 10.1246/cl.170011
Buyu Kou 1 , Wei Zhu 1 , Haixia Liu 1 , Hong C. Shen 1 , Jie Wu 2 , Taishan Hu 1
Affiliation  

This manuscript depicts efficient synthesis of structurally novel morpholine amino acids, (1S,4S)-2-oxa-5-azabicyclo[2.2.1]heptane-4-carboxylic acid (+)-1, its enantiomer (−)-1, and racemic (endo)-5-oxa-2-azabicyclo[2.2.1]heptane-3-carboxylic acid (±)-2, which could serve as compact modules in medicinal chemistry to potentially modulate physicochemical and pharmacokinetic properties of drug candidates, and to introduce intellectual properties.

中文翻译:

作为药物化学紧凑模块的桥连双环吗啉氨基酸的合成

这份手稿描述了结构新颖的吗啉氨基酸的有效合成,(1S,4S)-2-oxa-5-azabicyclo[2.2.1]heptane-4-羧酸 (+)-1,它的对映异构体 (-)-1,和外消旋 (endo)-5-oxa-2-azabicyclo[2.2.1]heptane-3-羧酸 (±)-2,可作为药物化学中的紧凑模块,潜在地调节候选药物的理化和药代动力学特性,并引进知识产权。
更新日期:2017-04-05
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