Substrate-A Synthesis-Route

O
BocHN 1. EDC, NHS O O
OH OH
2.H 2N 5 BocHN OH OH
N 5
H Br
+
NO 2

O 1. EDC, NHS O
Na2CO3, OH
O OH 2.H2N OH
Aceton/H 2O O N
RF BocHN O H
N 5 BocHN O
H N 5
NO 2 H
NO 2

O OEtCN
NCEtO O P
O N N(i-Pr) 2
P Cl H
(i-Pr) 2N BocHN O
N 5
DIPEA H
NO 2
CH 2Cl 2

Oligosynthese
 Substrate-B Synthesis-Route b

O
O
HN NH O H2N
OH
O Route1 H H
O N ~40%
HN NH S
DCC/NHS
H H DMF O O
O
OH
S HN NH
O Route2 H H O
O H
O N
S OH
TSTU/DIPEA HN NH O H2N
DMF/Dioxane/ OH O
H H
O N 85%
S
O O

DCC: DIPEA: N

N C N

BF4
NHS: O
TSTU: O
N
HON
O N
N
O O