多肽合成中困难序列的缩合研究进展

时间:2025-03-09

非常详细的综述性文章

药学学报Acta

PharmaceuticaSinica

2007,42(2):111—117

.111.

综述

Recentprogressinthe

improvementofthecouplingefficiency

of“difficult

sequences"inpeptidesynthesis

HANXiang,WANGDe—xin+

(InstituteofMateriaMedica,ChineseAcademyofMedicalSciencesandPekingUnionMedicalCollege,Beijing100050,China)

Abstract:EventhoughchemistryisnOWinplacethatpotentiallyallowshighcouplingefficiencies

beattained,successfulcouplingisusuallyinpeptide

synthesis.Somefactors

that

to

challengewhenSO—called‘‘difficultsequences”isenc!ountered

have

been

discussed

and

related

affectthecouplingefficiency

methodstoovercomethoseobstacleshavebeenintroducedinpresentreview.All

suggestionsproposedhere

are

valuableandalsofeasibleto

improvethe

couplingcompletenessinbothliquid..phase

Ot

solid..phase

peptidesynthesis.

Keywords:peptidesynthesis;couplingefficiency;difficultsequences;口.structureofpeptide

CLC

number:R916Documentcode:A

Article

ID:0513—4870(2007)02一0111—07

多肽合成中“困难序列"的缩合研究进展

香,王德心+

(中国医学科学院、中国协和医科大学药物研究所,北京100050)

摘要:化学学科发展至今拥有极强的能力来获得高的合成效率,但是在多肽合成中“困难序列”的存在仍然成为成功缩合的巨大挑战。本文综述了影响多肽缩合效率的因素以及提高“困难序歹旷缩合效率的有效方法。所述方法均简便易行,适用于多肽的固相合成或液相合成。

关键词:多肽合成;缩合效率;困难序列;口一构象

The

long

phenomenon

of“difficultin

their

sequences”has

to

residuesfromdue

the

to

resinexistintra

or

interchain

frustratedchemistsefforts

assemble

or

aggregationto

hydrogenbonds,producingdifficulty

the

occurrence

peptidescontainingsuch

sequences

bysolid

liquidcouplingreaction。“.Although

and

phasesynthesisprotocols。1’….Theconventionalcouplingmethods,such

as

severity

of“difficult

sequences”cannot

bepredicted

activeesterand

acid—anhydride

are

withconfidence,itisgenerallythoughtthatarisesfromthe

intermolecular

into

association

sometimesfailed

to

overtomethatobstacle[3I.The

not

use

ofresin.bound

structures

peptideduringthe

N—

ofnewcouplingreagentissynthesis,because

reactantsin

or

alwaysfruitfulinpeptidefrom

the

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