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ATTACHMENT AND ELABORATION STRATEGIES FOR INVERSE PEPTIDE SYNTHESIS
ATTACHMENT AND ELABORATION STRATEGIES FOR INVERSE PEPTIDE SYNTHESIS
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机译：反相肽合成的附着和合成策略
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摘要
The present invention provides a process for preparing a peptide of formula (I): Sub-[L]-[N(R1)-A-C(O)]p—[NH-A-C(O)]n+m—OH (I) comprising: (a) reacting an immobilized compound of formula (II): Sub-(L)-[N(R1)-A-C(O)]p—[NH-A-C(O)]n—OH (II) with an amino acid ester or peptide derivative of formula (III): H—[NH-A-C(O)]m—O(tBu) (III) in the presence of a coupling agent to yield a peptide compound of general formula (IV): Sub-[L]-[N(R1)-A-C(O)]p—[NH-A-C(O)]n+m—O(tBu) (IV); (b) removing the tBu (t-butyl) group to produce a solid-support bound carboxylic acid or peptide derivative of general formula (I); wherein n is a positive integer, e.g., 1-10, preferably 1-5; m is a positive integer, and P is 0-1.
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机译：本发明提供了制备式（I）的肽的方法：<？in-line-formulae description =“ In-line Formulae” end =“ lead”？> Sub- [L]-[N（R 1 ）-AC（O）] p -[NH-AC（O）] n + m -OH（I）<？in-line-formulae description =“在线表达式” end =“ tail”？ >包括：（a）使固定的式（II）化合物反应：<？in-line-formulae description =“ In-line Formulae” end =“ lead”？> Sub-（L）-[N（R 1 ）-AC（O）] p -[NH-AC（O）] n -OH（II）<？in-line-formulae description =“ In-line Formulae” end =“ tail”？>与式（III）的氨基酸酯或肽衍生物：<？in-line-formulae description =“在线公式” end =“ lead”？> H- [NH-AC（O）] m -O（tBu）（III）<？ in-line-formulae description =“在线公式” end =“ tail”？>在偶联剂的存在下产生通式（IV）的肽化合物：<？in-line-formulae description =“ In-line Formulae” end =“ lead”？> Sub- [L]-[N（R 1 ）-AC（O）] p — [NH-AC（O）] n + m —O（tBu）（IV）; <？in-line-formulae description =“在线公式” end =“ tail”？>（b）除去tBu（叔丁基）基团以产生固相结合的羧酸或通式（I）的肽衍生物;其中n是一个正整数，例如1-10，优选1-5。 m为正整数，P为0-1。
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