Synthesis of camptothecin melantotransferrin (p97) conjugate through a carbamate bond

被引：4

作者：

Chen, QQ ^{[1
]}

Gabathuler, R ^{[1
]}

机构：

[1] Biomarin Pharmaceut Inc, Novato, CA 94949 USA

来源：

SYNTHETIC COMMUNICATIONS | 2004年 / 34卷 / 13期

关键词：

camptothecin; melanotransferrin; brain tumor; blood-brain barrier; drug delivery; bioconjugate;

D O I：

10.1081/SCC-120039495

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Through its 20-hydroxy group and a carbamate bond, 20(S)-camptothecin (1) is chemically linked to melanotransferrin (p97). The key step to modify the steric hindered hydroxy group of camptothecin is achieved by using triphosgene/DMAP in DMF and immediately reacting with tert-butyl 6-aminohexanoate (8). The novel camptothecin conjugate 4 is a potential agent for chemotherapy of brain tumor.

引用

页码：2415 / 2424

页数：10

共 19 条

[1]

Begley DJ, 2000, BLOOD-BRAIN BARRIER AND DRUG DELIVERY TO THE CNS, P93

[2]

CARTER HE, 1967, ORG SYNTH, V3, P167

[3] Efficient one-pot synthesis of doxorubicin conjugates through its amino group to melanotransferrin p97 [J].