process for the production of 3 - glucos 2 yl) - desmethylthiocolchicin and 2 - glucos 2 yl) - desmethylthiocolchicin

摘要

3-Glucose-2-yl-3-demethyl-thiocolchicine(thiocolchicoside) and the 2-glucose-2-yl-2-demethyl-deriv. are prepd. by (i) reacting thiocolchicine (T) with BBr3 to give 1,2- and 2,3-bis-demethyl-T (the latter predominating); (ii) reacting with acetobromoglucose in the presence of a tertiary base to give 2- and 3-tetraacetoglucose-2-yl-2,3-bis-demethyl-T and 2-tetraacetoglucose-2-yl-1,2-bis-demethyl-T; (iii) reacting with CH3N2 then a base, and (iv) separating the mixture of the two products obtd. The five named inters. are new.