发明名称 |
METHOD OF ARALKYLATION OF 4'-HYDROXYL GROUP OF ANTHRACYCLINS |
摘要 |
A method for the aralkylation of anthracyclins by utilizing an aralkylating agent R3-CH2X (for example, BnBr) in accordance with the reaction pathway describe by the scheme shown in Fig. 1. The present invention recognizes that 4-R1, 3'-N3-Daunomycines are suitable substrates for selective 4'-O-benzylation, yielding 4-R1, 3'-N3-4 '-O-Aralkyl-Daunorubicines (in particular, 4'-O-Bn-Daunomycines). Thus, the present invention provides a pathway for a simple production of 4'-O-aralkylated derivatives of anthracyclines which can be effectively used to produce anthracyclines. |
申请公布号 |
WO2009088618(A1) |
申请公布日期 |
2009.07.16 |
申请号 |
WO2008US86088 |
申请日期 |
2008.12.09 |
申请人 |
SOLUX CORPORATION;ZABUDKIN, ALEXANDER;MATVIENKO, VICTOR;MATVEEV, ALEXEY;ITKIN, ALEKSANDR |
发明人 |
ZABUDKIN, ALEXANDER;MATVIENKO, VICTOR;MATVEEV, ALEXEY;ITKIN, ALEKSANDR |
分类号 |
A01N43/04;A61K31/70;C07H15/24 |
主分类号 |
A01N43/04 |
代理机构 |
|
代理人 |
|
主权项 |
|
地址 |
|