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Relevant academic research and scientific papers

Preparation of a camptothecin derivative by intramolecular cyclisation

PCT No. PCT/US95/05427 Sec. 371 Date Nov. 1, 1996 Sec. 102(e) Date Nov. 1, 1996 PCT Filed May 2, 1995 PCT Pub. No. WO95/29919 PCT Pub. Date Nov. 9, 1995The present invention relates to a method for the preparation of camptothecin and camptothecin-like compounds and to novel intermediates used in this preparation. In particular, the invention provides a process for the preparation of the camptothecin derivative of formula (I') known by the chemical name "7-(4-methylpiperazino-methylene)-10,11-ethylenedioxy-20(R,S)-camptothecin", which comprises cyclising the compound of formula (II'), wherein X is halogen, particularly chloro, bromo, or iodo; and when the compound of formula (I') is obtained as a mixture of enantiomers optionally resolving the mixture to obtain the desired enantiomer, and/or if desired, converting the resulting compound of formula (I') or a salt thereof into a physiologically acceptable salt or solvate thereof.

Intermediates in pharmaceutical camptothecin preparation

A process of providing novel compounds of Formula (I) below, which are useful as intermediates in the preparation of camptothecin and camptothecin-like compounds, STR1 wherein: R1 represents alkyl, particularly methyl, R2 represents H or alkyl, particularly methyl, R3 represents H or alkyl, particularly H; Q represents triflate or halo particularly bromo and iodo more particularly iodo and Y represents H, chloro or OR4, wherein R4 represents alkyl or triflate, or particularly H.

Catalytic enantioselective synthesis of 20(S)-camptothecin: A practical application of the sharpless asymmetric dihydroxylation reaction

The first catalytic asymmetric route to 20(S)-camptothecin was achieved, using as the key steps a tandem intramolecular Heck reaction/olefin isomerization process and a Sharpless asymmetric dihydroxylation (AD) reaction.