CAS: 7355-18-2; (2S,3R,4S,5S,6S)-6-(Methoxycarbonyl)Tetrahydro-2H-Pyran-2,3,4,5-Tetrayl Tetraacetate

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D-Glucurono-6,3-Lactone置于吡啶,三乙胺体系中,化学反应 122.0H,反应生成 1,2,3,4-四-O-乙酰基-β-D-葡萄糖醛酸甲酯
参考文献:1-O-(4-羟基甲基苯丙胺基)-α-D-吡喃葡萄糖醛酸甲酯的合成.
标题:1-O-(4-羟基甲基苯丙胺基)-α-D-吡喃葡萄糖醛酸甲酯的合成.
摘要:为直接表征甲基苯丙胺(ma)滥用者尿液中的完整结合形式,从市售的甲基4合成了对应于ma代谢产物之一的4-羟基甲基苯丙胺(4-Ohma)葡萄糖醛酸酯.-羟基苯乙酸.
DOI:10.1248/cpb.53.684

专利信息

专利号:US-9353140-B2
优先权日:2009-11-25
标 题:BQC-G, a tumor-selective anti-cancer prodrug
发明人：PRIJOVIC ZELJKO M; LEU YU-LIN; ROFFLER STEVE R
权利人:PRIJOVIC ZELJKO M; LEU YU-LIN; ROFFLER STEVE R; ACADEMIA SINICA
摘要:The invention relates to the synthesis of a second-generation camptothecin glucuronide prodrug (BQC-G) of a potent anticancer camptothecin derivative 5,6-dihydro-4H-benzo[de]quinoline-camptothecin (BQC). BQC-G was over 4000 times more water soluble than BQC, displayed good stability in human plasma and was an excellent substrate for enzymatic hydrolysis by bacterial and human β-glucuronidases. BQC-G was about 30 times less toxic than BQC, but was as toxic as BQC after hydrolysis of the glucuronide moiety by β-glucuronidase. In the presence of human serum albumin, BQC-G displayed lower cytotoxicity (IC 50 =1080 nM) but could be activated by β-glucuronidase to display potent activity (IC 50 =13.3 nM).

专利号:FR-2586687-A1
优先权日:1985-08-30
标题 :SYNTHESIS PROCESS AND NOVEL DERIVATIVES OF A, L-IDURONIC ACID