多肽合成中困难序列的缩合研究进展(6)
时间:2025-03-10
时间:2025-03-10
非常详细的综述性文章
116
药学学报Acta
PharmaceuticaSinica
2007,42(2):111—117
yields
fortherapidSPPS.using
Boc—aminoacid
derivatives,of
CGRP(human一Ⅱ.caleitonin
gene—
relatedpeptide)(8—37).They
observed
that
coupling
yields
are
highly
dependent
on
thesolventused.Maximumresinsolvationoccurred
with
NMP.
NMP—DMSO(8:2)andDMSO.Inefficientsolvationof
the
peptide—resin
occurred
with
these
solvents
and
resultedinpoorsyntheseswithaveragecouplingyieldsof78.1。88.9and
91.8%.respectively.Superior
peptide—resin
solvationwas
obtainedusing
DMA
(dimethylacetamide)
and
DMF,
resultingin
significantlyhigheraveragecouplingyieldsof98.0and
2).
2
Average
couplingyieldsforthe
synthesisof
Solventsystem
Avg.coupling
yield/%
DMF
provided
themosteffective
peptide—resinand
was
theonly
solventfrom
whichCGRP
obtained
as
a
singlemajorproductinthe
cleavedmaterial.Itshouldpointout
thatunderconditions
the
peptidyl—resin
has
differentresponses
even
inthe
same
solvent.
solventnot
onlywiththechangeofchainlengthbutalso
withthe
alternation
of
stages
ineach
syntheticcircle.such
as
the
deprotecting
and
couplingsolvents,isnecessary
for
the
enhancement
of
coupling
Thus,the
success
of
SPPSisoften
dependent
solvationoftheresinandthegrowingresin—bound
chain.Theuse
ofnewsupports
thatincreaseseparation
and
peptide
chain
solvation
is
CLPSER(cross—linked
polystyrene—
acrylate
resin)。3“showed
excellent
in
a
broadrangeofsolventsused
in
SPPS.newresinwascomparedwithcommercialsupportsas
MerrifieldandSheppardresinsbysynthesizing
acylcarrier
protein(65—74)fragment
underthe
experimental
conditions.HPLC
(high—
liquid
chromatography)profiles
revealed
highefficiencyofthenewlydevelopedsupport.CM
3
(polyethylene
glyc01)一based
resin,performing
excellentlyfor
the
preparationofhydrophobic,highly
structured,andpoly—Argpeptides,ascomparedtoPS
(polystyrene)resins.Themechanis …… 此处隐藏:1945字,全部文档内容请下载后查看。喜欢就下载吧 ……