COUNOTTE-POTMAN A.; PLAS H. C. VAN DER; VELDHUIZEN B. VAN, J. ORG. CHEM., 1981, 46, NO 10, 2138-2141
作者:COUNOTTE-POTMAN A.、 PLAS H. C. VAN DER、 VELDHUIZEN B. VAN
DOI:——
日期:——
SUN, XI-CHENG;REN, GUO-DU, YUTSZU XUASYUEH, 8,(1988) N 4, S. 365-368
作者:SUN, XI-CHENG、REN, GUO-DU
DOI:——
日期:——
MULTIFUNCTIONALIZED POLYETHYLENE GLYCOL DERIVATIVE AND PREPARATION METHOD THEREFOR
申请人:XIAMEN SINOPEG BIOTECH CO., LTD.
公开号:US20170312363A1
公开(公告)日:2017-11-02
Disclosed are a multifunctionalized polyethylene glycol derivative and a preparation method therefor. The derivative has an H-shaped structure as represented by formula (1) and comprises one linear core LPEG and four PEG branch chains, where n
1
, n
2
, n
3
, and n
4
respectively are the degrees of polymerization of the branch chains, U
1
and U
2
are trivalent branching groups connecting the core LPEG to two of the PEG branch chains, F
1
and F
2
contain a functional group or a protected form R
01
thereof and may or may not contain a branched group G, correspondingly, the number of R
01
is one or more, F
1
and F
2
are either identical or different, any one linking group in the molecule or any linking group formed with an adjacent heteroatom group can either remain stable or be degraded, and any one PEG segment in the molecule is discretely polydispersed or monodispersed. The multifunctional polyethylene glycol is flexible and diverse in terms of branch structures and the lengths of branching arms, has various parameters and performance indicators that are adjustable and easy to control, and has a broad applicability.
EIGHT-ARM POLYETHYLENE GLYCOL DERIVATIVE, PRODUCTION METHOD THEREFOR, AND MODIFIEDBIO-RELATEDSUBSTANCETHEREOF
申请人:XIAMEN SINOPEG BIOTECH CO., LTD
公开号:US20180214561A1
公开(公告)日:2018-08-02
Disclosed are an eight-arm polyethylene glycol (PEG) derivative (formula I), production method therefor and modified bio-related substance thereby. Wherein, one tetravalent group U together with four trivalent groups E
c
form a highly symmetrical octavalent group CORE
0
; L
c
connects the octavalent group to eight PEG chains having polydispersity or monodispersity and having n
1
to n
8
as the degree of polymerization thereof; the terminal of one PEG chain is connected to at least one functional group F (k≥1); said PEG chain and F therebetween can be directly connected (g=0) or be indirectly connected via a linking group L
0
to a terminal end-branching group G (g=1); the latter provides more reactive sites for binding more drug molecules and increases the drug loading. The eight-arm polyethylene glycol derivative has a centrosymmetric or approximately centrosymmetric structure, and leads to more precise control of the molecular weight in large-scale production and much narrower distribution of molecular weight for products. The modified bio-related substance thereby has a more uniform and controllable performance.