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首页> 外文会议>Chinese peptide symposium >2,2-Difluoroboroxazolidin-5-ones: A novel approach to selective side-chain protections of serine and threonine by tert-butyl or benzyl groups
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2,2-Difluoroboroxazolidin-5-ones: A novel approach to selective side-chain protections of serine and threonine by tert-butyl or benzyl groups

机译：2,2-二氟呋喃唑唑胺-5-苯甲唑胺 - 一种新的叔丁基或苄基选择丝氨酸和苏氨酸的侧链保护方法

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摘要

In peptide synthesis, Boc and Fmoc chemistries are routine methods to obtain desired peptides. Traditionally, the side chain hydroxyl functions in Ser and Thr have been protected as benzyl (Bzl) ethers based on N alpha -Boc protection, and as tert-buty(t-Bu) ethers in combination with Fmoc group as the N alpha -protecting group. More recently, Fmoc-Ser(Bzl) and Fmoc-Thr(Bzl) have been employed in convergent solid phase peptide synthesis. However, methods for the preparation of these side-chain protected compounds are cumbersome [1-4]. We have obtained 1 (Scheme) from aspartic acid and glutamic acid, and reported the synthesis of Asp(t-Bu) and Glu(t-Bu) using 1 as intermediates which give a simultaneous protection of both alpha -function groups and are stable to Lewis acid catalysts [7]. In this paper, we describe an efficient and practical one-pot synthesis of the Bzl and t-Bu-based side-chain protected derivatives of serine and threonine.
机译：在肽合成中，BOC和FMOC化学物质是获得所需肽的常规方法。传统上，Ser和Thr中的侧链羟基官能团被视为基于Nα-中的苄基（BZL）醚，以及与FMOC组相结合的叔丁基（T-BU）醚作为Nα-保护团体。最近，FMOC-SER（BZL）和FMOC-THR（BZL）已用于收敛固相肽合成。然而，制备这些侧链保护化合物的方法是麻痹的[1-4]。我们已经获得了来自天冬氨酸和谷氨酸的1（方案），并报道了使用1作为中间体的ASP（T-BU）和Glu（T-Bu）的合成，其同时保护αfunction组并稳定Lewis酸催化剂[7]。在本文中，我们描述了丝氨酸和苏氨酸的基于BZL和T-BU的侧链保护衍生物的高效实用的单罐合成。

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