摘要 |
<p>NEW MATERIAL:The bicycloocane derivative of formula I (R1 and R3 are H or lower alkyl; R2 is H or 3-10C alkyl; X1 is CH=CR4 or CH2CHR4; R4 is lower alkyl, benzyl or aryl; Y1 and Y2 are H or OH-protecting group) or its pharmacologically permissible salt. EXAMPLE:2beta-( 3'beta- Hydroxy-2'-methyl- trans-1'-octenyl)-3alpha-hydroxy- 7 (Z)-( 4'-carboxybutylidene)-bicyclo(3,3,0)octane. USE:Antitumor agent having improved chemical stability and selectivity of action of PGI2. PROCESS:The compound of formula I is prepared by reacting the compound of formula II (Y'1 and Y'2 are H or OH-protecting group) with a Witting reagent of formula III (M is H or alkali metal; Ph is phenyl), if necessary, esterifying the carboxyl group, and if necessary, removing the protecting group from OH or protecting OH groups.</p> |