- PROCESS FOR THE CONVERSION OF COLCHICINOIDS TO THEIR 3-GLYCOSYLATED DERIVATIVES VIA THEIR RESPECTIVE 3-DEMETHYL ANALOGUES
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The present invention relates to a bioprocess for the preparation of glycosylated Colchicine, its analogs and derivatives of formula (I) wherein X represents O or S, and R1 represents C1-C6 alkyl, R2 is a glycoside residue, R represents hydrogen, C1-C6 alkyl, formyl or acetyl.
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Page/Page column 12; 13
(2015/07/15)
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- "Process for the glycosidation of colchicine and thiocolchicine"
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A process for the preparation of compounds having formula I is disclosed, wherein: - R1 is a methoxy or methylthio group; - R2 is a O-glycosyloxy residue. Compounds having formula I are prepared by reacting the corresponding precursor having R2 = OH and the suitably protected 1-acetyl-glycose.
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Page/Page column 3-4
(2009/12/23)
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- Novel 3-O-glycosyl-3-demethylthiocolchicines as ligands for glycine and γ-aminobutyric acid receptors
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New 3-O-glycosyl-3-demethylthiocolchicines containing natural and unnatural sugar moieties were prepared and tested on γ-aminobutyric acid (GABA) and strychnine-sensitive glycine receptors present in rat brain and spinal cord. Two different synthetic approaches were used with the readily available 3-O-demethylthiocolchicine (1b) and thiocolchicoside (2a). Glycosyl compounds 2a-g were obtained from 1b and 1-fluorosugars 4. 6′-Heterosubstituted glycosyl compounds 6-12 and the 6′-desoxy derivative 2h were prepared from 2a.
- Gelmi, Maria Luisa,Fontana, Gabriele,Pocar, Donato,Pontremoli, Guido,Pellegrino, Sara,Bombardelli, Ezio,Riva, Antonella,Balduini, Walter,Carloni, Silvia,Cimino, Mauro
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p. 2245 - 2248
(2008/02/01)
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- Process for the glycosidation of colchicine derivatives and the products obtained thereby
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A process for the preparation of compounds having the formula STR1 wherein: R is a methoxy or thiomethyl group; R1 is a β-D-glycopyranosyloxy or 6-deoxygalactopyranosyloxy residue; and R2 is a C1 -C7 alkyl group which process comprises reacting a protected material selected from the group consisting of derivatives of 1-fluoroglucose and 1-fluorofucose with a compound having the formula STR2 wherein R and R2 are as defined above to form a crude reaction product containing at least one compound of formula (I).
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- A process for the glycosidation of colchicine derivatives and products obtained
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The present invention relates to a process for the preparation of colchicine or thiocolchicine glycosides or derivatives thereof.
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