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    • 4. 发明授权
    • Methods for preparing Irinotecan
    • 伊立替康的制备方法
    • US07683170B2
    • 2010-03-23
    • US11608946
    • 2006-12-11
    • Friedrich WissmannHolger RauterSilvia Werner
    • Friedrich WissmannHolger RauterSilvia Werner
    • C07D489/00
    • C07D491/22
    • Methods for manufacturing 7-ethyl-10-[4-(1-piperidino)-1-piperidino]-carbonyloxy-camptothecin are described comprising I. reacting a mixture of 1-chlorocarbonyl-4-piperidinopiperidine hydrochloride and 7-ethyl-10-hydroxycamptothecin in a polar aprotic solvent with a base in the presence of catalytic amounts of a N-containing cyclic organic compound having 3 to 20 carbon atoms and optionally in the presence of a water binding agent in an amount which effectively binds any water present in the above reactants and solvents; or II. reacting: (a) 7-Ethyl-10-hydroxycamptothecin in a polar aprotic solvent with phosgene, trichlormethyl-chloroformate, bis(trichloromethyl)carbonate or a alternative to phosgene and a base in the presence of catalytic amounts of a N-containing cyclic organic compound having 3 to 20 carbon atoms; and (b) subsequently with piperidinopiperidine and an amine base.
    • 描述了制备7-乙基-10- [4-(1-哌啶子基)-1-哌啶子基]羰基氧基喜树碱的方法,其包括:将1-氯羰基-4-哌啶基哌啶盐酸盐和7-乙基-10- 羟基喜树碱在极性非质子溶剂中与碱在催化量的含3-20个碳原子的含N环状有机化合物存在下,任选地在水结合剂存在下,其量有效地结合存在于 以上反应物和溶剂; 或II。 反应:(a)在极性非质子溶剂中的7-乙基-10-羟基喜树碱在光气,三氯甲基氯甲酸酯,双(三氯甲基)碳酸酯或碳酰氯和碱的替代物存在下,在催化量的含氮环状有机物 具有3-20个碳原子的化合物; 和(b)随后与哌啶基哌啶和胺基。