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R = -OC(=O)Ph
R = -OH
R = -N(+)Et
3Na
N
3DMF
Na
N
3DMF
, toluene, 40 C , toluene, 40 C CuBr, HMTETA or Me6TREN DMF, 60 C CuI, DBU THF, 35 CmCPBA
Hydrophilic polyester
Hydrosoluble cationic
polyester
applications : gene therapy
and antibacterial properties
conv : 95% (Me
6TREN)
40% (HMTETA)
conv : 30% (HMTETA)
95% (Me
6TREN)
conv : 30% (HMTETA)
conv : 42% (HMTETA)
R = -CH
2OC(=O)Ph
R = -CH
2OH
R = -CO
2H
R = -CH
2-epoxide
(CH2)4 O O (CH2)5 O O x Cl yz CO2-PEO-OMe N(+)Me2-PEO-OH1) Na
N
3, DMF
2)
ATRA route
Click route
- conversion around 30% whatever the route used
- purification of the polymer by dialysis
- forms micelles in water as evidenced by light scattering and TEM
-
Application:
the graft copolymer is a stabilizer for the preparation of
stealth nanoparticules for drug delivery applications.
quantitative conversion in all cases
α
αα
α
polymer matrix (PDLLA)
poly(CL-g-EO)
30 mol% of azide groups Mnaround 10000 50 mol% of Cl groups Mnaround 10000 O Sn O Bu Bu O SnO Bu Bu DSDOP(Initiator) DSDOP(Initiator)
70%
!" (CH2)4 O O (CH2)5 O O x yz Cl CO2-PEO-OMe N N N (CH2)4 O O (CH2)5 O O x yz N(+)Me2-PEO-OH O O O Cl O x yz O O O O x yz N3 N N N O O O O x yz R O O O O x yz R Clyield: 50%
PhL and ChJ-A are assiociate researchers by the belgian # FNRS $. RR thanks the #Fonds pour la Formation % la Recherche dans l&Industrie et L&Agriculture $ ( FRIA) for financial support. The authors are indebted to the #Belgian Science Policy $ for financial support in the frame of #Interuniversity Attraction Poles Programme (PAI V/03)$.
