110351-94-5Relevant articles and documents
Synthetic studies on camptothecins. Part 3
Kuang, Yun-Yan,Niu, Jing-Ze,Chen, Fen-Er
, p. 2094 - 2099 (2010)
A concise and efficient asymmetric process for the total synthesis of (20S)-7-ethyl-10-hydroxycamptothecin (=SN-38; 1f), an active metabolic form of the prodrug irinotecan, is described. This approach features the enantioselective cyanosilylation of indolizinone 4 into the corresponding cyanohydrin 5, mediated by a bifunctional thiourea-based cinchona alkaloid under mild conditions, and I2-catalyzed Friedlnder condensation of the tricyclic lactone 6 and 2-amino-5-hydroxy propiophenone (=1-(2-amino-5- hydroxyphenyl)propan-1-one). Copyright
Enantioselective synthesis of 20(S)-camptothecin using an enzyme- catalyzed resolution
Imura, Akihiro,Itoh, Motohiro,Miyadera, Akihiko
, p. 2285 - 2291 (1998)
The important key intermediate of a 20(S)-camptothecin synthesis was prepared enantioselectively using an enzyme-catalyzed resolution. A commercially available papain was found to exhibit the highest enantioselectivity with moderate activity, and the (S)-enantiomer of 99% ee was obtained as the remaining substrate.
Camptothecin derivative and preparation method and application thereof
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Paragraph 0223-0227; 0250-0253, (2020/01/03)
The invention relates to a compound with a structure shown in a formula (I), a stereoisomer of the compound and a pharmaceutically acceptable salt form of the compound, and further relates to a preparation method of the compound, a pharmaceutical composition containing therapeutically effective dose of the compound, and application of the pharmaceutical composition in the preparation for the prevention and/or treatment of cancer. The compound is a camptothecin derivative with a novel structure with 10 site and 11 site of a stem nucleus introduced with methylene dioxy groups and 7-site introduced with different substituted groups. The raw materials of the preparation method can be obtained easily, a synthetic method is simple, a purification method is simple and fast, the compound has excellent cytotoxic activity in vitro and excellent antitumor effect in vivo, and the compound has broad medicinal prospects.(Please see the specification for the formula).
COMPOUND OF CAMPTOTHECIN AND PREPARATION AND USE THEREOF
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Paragraph 0097, (2015/05/05)
The present disclosure relates to a compound of formula I, a pharmaceutical composition thereof and the use thereof as an anti-tumor drug.