PURPOSE: To obtain an ethylenically unsatd. bile acid deriv. having an ethylenically unsatd. group bonded to a bile acid deriv. through a bridge group and used as starting material for the preparation of a polymeric bile acid deriv. which inhibits the re-absorption of bile acid in the small intestine and is useful as a lipid in blood degradation medicine.
CONSTITUTION: A bile acid deriv. of formula I [where R3 to R8 are each H, (protected) OH or ON2; and B is OH, an O-alkali metal, O-alkaline earth metal, O-1-12C alkyl, O-allyl or the like] is sulfonylated by reaction with methanesulfonyl chloride or the like, a bridge group is introduced by reaction with an ω-alkanediol under heating in the presence of a base and the resultant compd. is sulfonylated by reaction with methanesulfonyl chloride, azidated by reaction with sodium azide or the like, derived to an amino group by reduction with a Pd catalyst and then allowed to react with acrylic acid chloride, maleic anhydride or the like to obtain the objective ethylenically unsatd. bile acid deriv. of formula II (where G is the bile acid deriv. of the formula I; X is the bridge group; and A is a polymerizable ethylenically unsatd. group).
HAINAA GUROMUBIKU
SHIYUTEFUAN MIYURUNAA
GIYUNTAA BUESU
