| 摘要 |
<p>PURPOSE: Provided is a novel intermediate compound obtained in a process for preparing optically active or racemic colchicine and thiocolchicine and analogues and derivatives thereof. CONSTITUTION: The intermediate is represented by formula (F2), wherein G1 is H or R'''1 radical; (a) R'''1 and R'''2 are both alkyl groups and R'"3 is A-SO2-, (b) R'''2 and R''' are both alkyl groups and R''' is A-SO2-, (c) R'''1, R'''2 and R''' are alkyl groups, (d) R'''1 is A-SO2- and R'''2 and R'''3 together with the oxygen atom to which they are attached, form -O-X-O- (in which X is a group represented by the formula of -B(OCR5R6)-, R5 and R6 are individually selected from the group consisting of H, an alkyl, phenyl or a substituted phenyl, or R5 and R6 together with the carbon atom to which they are attached form a 5- or 6-membered carbocyclic group); or (e) R'''3 is A-SO2- and R'''1 and R'''2 together with the oxygen atom to which they are attached form -O-X-O-; A is selected from the group consisting of an alkyl, phenyl non-substituted or substituted by 1 to 3 of alkyl groups and naphthyl non-substituted or substituted by 1 to 5 of alkyl groups; Rc and Rd are identical or different and represent H or OH; and the dotted line represents a double or single bond. The compound has the form of an (R)-isomer, an (S)-isomer or a mixture thereof.</p> |
