A comparison study of synthesizing methods of thiolated dxooru bicin
10.3969/j.issn.1006-0111.2014.06.008
- VernacularTitle:巯基化阿霉素的两种合成方法的比较
- Author:
Shan WU
1
;
Yeye ZHANG
;
Haixia GUO
;
Junjie LIU
;
Zhiguo SUN
;
Yanqiang ZHONG
;
Hao ZOU
Author Information
1. 第二军医大学药学院药剂学教研室
- Keywords:
thiolated doxorubicin;
2-iminothiolane (2-IT);
S-acetylthioglycolic acid N-hydroxysuccinimide ester (SATA)
- From:
Journal of Pharmaceutical Practice
2014;(6):428-433
- CountryChina
- Language:Chinese
-
Abstract:
Objective To investigate the optimal method for synthesizing thiolated doxorubicin .Methods Thiolated doxorubi-cin was synthesized through two different methods .Doxorubicin was reacted with 2-iminothiolane (2-IT) and S-acetylthioglycolic acid N-hydroxysuccinimide ester (SATA),respectively.The synthesized thiolated doxorubicin was further characterized by HPLC and MS -ESI techniques .Several factors including molar ratios as well as reaction time were evaluated .Results The results showed that thiolat-ed doxorubicin could be synthesized via both of the two methods successfully .Thiolated doxorubicin could be stable when doxorubicin was reacted with SATA .But the crude thiolated doxorubicin could be cyclized easily when doxorubicin was reacted with 2-IT.Conclu-sion Thiolated doxorubicin prepared with SATA is more feasible than that with 2-IT.
