Photo-induced preparation of unnatural α-amino acids: synthesis and characterization of novel Leu5-enkephalin analogues,Organic Chemistry Frontiers

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Photo-induced preparation of unnatural α-amino acids: synthesis and characterization of novel Leu5-enkephalin analogues
Organic Chemistry Frontiers ( IF 4.6 ) Pub Date : 2020-07-28 , DOI: 10.1039/d0qo00696c
Hongxiang Xue _{1,

2,

3,

4,

5} , Mengzhun Guo _{3,

4,

6,

7,

8} , Chao Wang _{3,

4,

6,

7,

8} , Yuxuan Shen _{1,

2,

3,

4,

5} , Rupeng Qi _{3,

4,

6,

7,

8} , Yifei Wu _{1,

2,

3,

4,

5} , Zhaoqing Xu _{3,

4,

6,

7,

8} , Min Chang _{1,

2,

3,

4,

5}

Affiliation

We here report the first example of the photo-induced preparation of unnatural α-amino acids and modification of peptides with unactivated alkyl chlorides (iodides) without the assistance of a transition metal catalyst or photosensitizer. The method was successfully applied for the late-stage modification of peptides and provided a novel enkephalin analogue with significantly better analgesic activity and 2.6-fold more long-lasting time compared to its parent peptide.

中文翻译：

光诱导的非天然α-氨基酸的制备：新型Leu5-脑啡肽类似物的合成与表征

我们在这里报告了第一个例子，说明了在不借助过渡金属催化剂或光敏剂的情况下，光诱导制备非天然α-氨基酸和用未活化的烷基氯（碘化物）修饰肽的方法。该方法已成功应用于肽段的后期修饰，并提供了一种新型脑啡肽类似物，其镇痛活性明显优于其母体肽，并且持久时间延长了2.6倍。

更新日期：2020-08-25

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