发明名称 |
METHODS OF CHEMICAL SYNTHESIS OF PHENOLIC NITROGEN MUSTARD PRODRUGS |
摘要 |
This invention pertains to novel methods for the synthesis of certain nitrogen mustard prodrugs, such as N-{4-[N,N-bis(2-haloethylamino)-phenoxycarbonyl}-L-glutamic acid: wherein: X2 is a halo group, and is -F, -Cl, -Br, or -I; n is an integer from 0 to 4; and, each RA is an aryl substituent. The methods comprise, at least, the steps of: glutamate conjugation (GC); silyloxy deprotection (SD); and, sulfonic esterification (SU). Certain preferred methods comprise the steps of: amine substitution (AS); silyloxy protection (SP); phenolic deprotection (PD); activation (AC); glutamate conjugation (GC); silyloxy deprotection (SD); sulfonic esterification (SU); halogenation (HL); glutamate deprotection (GD); and glutamic acid protection (GP).
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申请公布号 |
WO02060862(A1) |
申请公布日期 |
2002.08.08 |
申请号 |
WO2002GB00281 |
申请日期 |
2002.01.24 |
申请人 |
CANCER RESEARCH CAMPAIGN TECHNOLOGY LIMITED;SPRINGER, CAROLINE, JOY;NICULESCU-DUVAZ, DAN |
发明人 |
SPRINGER, CAROLINE, JOY;NICULESCU-DUVAZ, DAN |
分类号 |
C07C269/04;C07C271/54;C07C303/28;C07C309/66;C07F7/18;(IPC1-7):C07C269/04 |
主分类号 |
C07C269/04 |
代理机构 |
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地址 |
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