143655-58-7Relevant articles and documents
Intermediate for synthesizing camptothecin derivative as well as preparation method and application thereof
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, (2020/08/09)
The invention relates to the technical field of organic compound synthesis, in particular to an intermediate for synthesizing a camptothecin derivative as well as a preparation method and applicationof the intermediate. An intermediate A can be obtained by acylation, bromination and cross coupling reaction of 3-fluoro-4-methylaniline. The intermediate A can be used for preparing an intermediate Bso as to further prepare Exatecan mesylate. The intermediate compound B can be obtained by rearrangement reaction of the intermediate A; Exatecan mesylate can be obtained by subjecting the intermediate compound B to alpha-site acetamido and amino deprotection, condensation reaction and hydrolysis reaction. The method has the advantages of low price of reaction initiators, mild reaction conditionsof each step, simplicity and convenience in operation, high yield and suitability for industrial production.
Aminotetralone derivatives and preparation process thereof
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, (2008/06/13)
The present invention pertains to a process for the preparation of Compound (4) through the below-described reaction route: STR1 wherein R1 and R2 each represents H, halogen, OH or C1-6 alkyl group; X and Y each represents a protected amino group and n stands for 0 to 4. According to the above process, an aminotetralone derivative which is an intermediate useful for an industrial preparation of a camptothecin derivative can be obtained in a convenient manner and in a high yield.
Synthesis and antitumor activity of ring A- and F-modified hexacyclic camptothecin analogues
Sugimori, Masamichi,Ejima, Akio,Ohsuki, Satoru,Uoto, Kouichi,Mitsui, Ikuo,Kawato, Yasuyoshi,Hirota, Yasuhide,Sato, Keiki,Terasawa, Hirofumi
, p. 2308 - 2318 (2007/10/03)
Nineteen ring A- and F-modified hexacyclic analogues of camptothecin were synthesized by Friedlander condensation of appropriately substituted bicyclic amino ketones with tricyclic ketone and were evaluated for cytotoxicity and topoisomerase I inhibitory
Hexa-cyclic compound
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, (2008/06/13)
A novel hexa-cyclic compound, a derivative of camptothecin, of the general formula: STR1 The compound is prepared from an aminoketone compound and a pyranoindolizine compound by the condensation-ring closing reaction. It is abundantly water-soluble, and has an excellent antitumour activity and a high degree of safety, and can be applied as an antitumour medicine for curing tumors of various kinds.