【药物名称】Gimatecan, LBQ-707, CPT-184, ST-1481
化学结构式(Chemical Structure):
参考文献No.44941
标题:Camptothecin derivs. having antitumor activity
作者:Carminati, P.; Penco, S.; Zunino, F.; Merlini, L. (Istituto Nazionale per lo Studio e la Cura dei Tumori; Sigma-Tau Industrie Farmaceutiche Riunite SpA)
来源:EP 1044977; WO 0053607
合成路线图解说明:

Radical hydroxymethylation of camptothecin (I) by means of MeOH in the presence of H2O2 and FeSO4 provided (II). Subsequent heating of alcohol (II) in acetic acid gave rise to 7-formylcamptothecine (III). Finally, condensation of aldehyde (III) with O-t-butylhydroxylamine afforded the corresponding oxime.

合成路线图解说明:

The title imine derivative was prepared by condensation of the known 7-formylcamptothecin (I) with aniline (II) in the presence of ytterbium triflate and molecular sieves in CH2Cl2.

参考文献No.170378
标题:Chemical modification of an antitumor alkaloid camptothecin: Synthesis and antitumor activity of 7-C-substituted camptothecins
作者:Sawada, S.; Nokata, K.; Furuta, T.; Yokokura, T.; Miyasaka, T.
来源:Chem Pharm Bull 1991,39(10),2574
合成路线图解说明:

Semisynthesis: Treatment of camptothecin (XI) with tert-butylhydroperoxide in the presence of FeSO4, conc. H2SO4 and acetic acid in water gives (S)-7-methylcamptothecin (XII). Mannich reaction of compound (XII) with isopropylamine hydrochloride in DMSO as a formaldehyde source gives CKD-602.

合成路线图解说明:

Radical hydroxymethylation of camptothecin (I) by means of MeOH in the presence of H2O2 and FeSO4 provided (II). Subsequent heating of alcohol (II) in acetic acid gave rise to 7-formylcamptothecine (III). Finally, condensation of aldehyde (III) with O-t-butylhydroxylamine afforded the corresponding oxime.

参考文献No.633493
标题:Novel 7-oxyiminomethyl derivatives of camptothecin with potent in vitro and in vivo antitumor activity
作者:Dallavalle, S.; Ferrari, A.; Biasotti, B.; Merlini, L.; Penco, S.; Gallo, G.; Marzi, M.; Tinti, M.O.; Martinelli, R.; Pisano, C.; Carminati, P.; Carenini, N.; Beretta, G.; Perego, P.; De Cesare, M.; Pratesi, G.; Zunino, F.
来源:J Med Chem 2001,44(20),3264
合成路线图解说明:

Radical hydroxymethylation of camptothecin (I) by means of MeOH in the presence of H2O2 and FeSO4 provided (II). Subsequent heating of alcohol (II) in acetic acid gave rise to 7-formylcamptothecine (III). Finally, condensation of aldehyde (III) with O-t-butylhydroxylamine afforded the corresponding oxime.

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