PURPOSE: To economically obtain the subject compd. showing therapeutic activity without producing by-products by a new method of inverting a specified starting compd. into a halohydrin, rearranging the halohydrin in the presence of an alcohol, and treating the rearranged product with an acid.
CONSTITUTION: First, a compd. expressed by formula I is inverted into a halohydrin expressed by formula V (X is a halogen). In formula I, R is H, ester residue or the like; R' is methyl, CH2-OR" (R" is ester or ether residue); rings A', B' are formula II or formula III (K is 0, formula IV or the like; (n) is 2, 3; K" is a 1-8C alkyl or a 6-12C aryl) or the like. Then the halohydrin is subjected to rearrangement in the presence of an alcohol (preferably ethylene glycol) preferably by heating at ≤100°C, and then treated with an acid to obtain the objective compd. expressed by formula VI (rings A and B are formula II). To invert the compd. of formula I into the compd. of formula V, for example, the compd. of formula I is reacted with N-bromsuccinimide and then a mixture of perchloric acid and water is added to the reaction mixture.
JIYAN BIYUANDEIA
KURISUTEIAN DEIORE
MISHIERU BIBA
