Preparation of prostaglandin analogues with more - specific biological activity than natural prostaglandins

摘要

Prostaglandin analogues (II) are new compds. prepared by reacting water at 0-60 C with disulphenic esters of formula I, which may have the exo- or endv configuration. (which n is 1-8; a is 0-4; R15 is C1-4 alkyl or -CH2CCl3: Y = i-butyl, t-butyl, 3,3- difluorobutyl, 4,4-difluorobutyl, or 4,4,4-triflurorbutyl; is approx. indicates that the -(CH2)n-COOR15 group is in alpha- or beta-configuration relative to the ring; R6 is C1-5 alkyl) Advantages/uses:- the cpds. II and III and their derivatives are analogous to prostaglandin E, prostaglandin F and prostaglandin A in their bilogical activity, but are much more specific in action. As the present compounds have a narrower biological spectrum, their use is generally attended by a lesser degree of undesired side actions than for the natural prostaglandins. In addition, some of the synthetic compounds show a higher biological response than the natural prostaglandins in a specific area.