非常详细的综述性文章
药学学报Acta
PharmaceuticaSinica
2007,42(2):111—117
available
impact
to
minimize
oreven
abolishthe
negative
alsosuccessfully
applied
to
theassemblyofpeptides
ofthe
these
use
sequencesduringsynthesis.These
reagents。…,
in
containingseveralsecondaryandhinderedamines.2
ReasonableroutesforfragmentscouplingSegmentscondensationis
synthesis
of
long
sequence
an
includewhich
ofgive
powerful
a
acylating
protocolssignificant
increasethefor
importantwayforthepeptide.
“Difficult
efficiencyofpeptide
chain
assembly,especially
‘‘difficultsequences”.Thepopularityofuroniumbasedcouplingreagents
for
peptide
synthesis
has
increasedthatproved
as
sequences”may
becircumventedbyadequatedefinition
correct
ofsegmentand
For
choiceofcondensationsite[9|.
can
significantly(Figure1).Certain
to
sequences
longpeptidessynthesis,thetargetpeptide
into
several
protected
were
or
be
bemore
difficult
to
synthesize,such
BoPrPdividedcarboxyl
fragments.Those
chosen
which
amino
(bovine
Prion
Protein)(90—200),were
a
successfullycomponents
Gly
to
generally
as
preparedusing
combinationofthe
highlyactivated
usuallycontainacid.in
order
Pro
the
C—terminal
couplingreagent
1,
HATU(O一(7-azabenzotrizole一1一y1)一
hexanuorophosphate)
total
of
and
et
minimizethe
possibleracemization
1,3,3一tetramethyluronium
duringtheshortfragmentssynthesis,andthen,口一sheet
was
not
(Figure
1)
t-Boc
(tert.butyloxycarbonyl)
synthesis
the
tendency
to
beformedinthe
produced
chemistry[3].Wu
al[7]reported
longer
intermediate㈨.In
should
otherword,whenthelonger
performed,the
at
human理一defensins4,5,and6,usingthe
optimizedneutraliza—
fragmentscondensationreactionswerePro
residue
be,if
of
DIEA(N,N—diisopropylethylamine)in
tetramethyluronium
activationreport
situ
possibly,locatedC—terminal
in
a
the
tion/HBTU(2一(1H—benzotriazol一1一y1)一1,1,3,3一
hexanuorophosphate)(Figure …… 此处隐藏:1717字,全部文档内容请下载后查看。喜欢就下载吧 ……