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专利信息
专利号:US-6916949-B2
优先权日:2001-01-29
标 题 :Methods of chemical systhesis of phenolic nitrogen mustard prodrugs
发明人:SPRINGER CAROLINE JOY; NICULESCU-DUVAZ DAN
权利人:CANCER REC TECH LTD
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 estenfication (SU); halogenation (HL); glutamate deprotection (GD); and glutamic acid protection (GP).
专利号:WO-02060862-A1
优先权日:2001-01-29
标题:Methods of chemical synthesis of phenolic nitrogen mustard prodrugs
专利号:EP-1355876-B1
优先权日:2001-01-29
标题:Methods of chemical synthesis of phenolic nitrogen mustard prodrugs
专利号:EP-1355876-A1
优先权日:2001-01-29
标题 :Methods of chemical synthesis of phenolic nitrogen mustard prodrugs