| 摘要 |
The present invention describes 5-fluoro-3-oxa-prostacyclin (PGI2) derivatives of Formula I. These compounds are useful for the treatment of platelet dysfunction, atherosclerosis, hypertension and tumor cell metastasis. Also disclosed is the process for preparing them and the appropriate intermediates. <IMAGE> I wherein R1 is: (a) Na, K, or 1/2 Ca, or other pharmaceutically acceptable cation (b) NR32, where R3=H, methyl, ethyl, isopropyl or a combination of these groups; (c) Alkyl of 1 to 6 carbon atoms, either branched or straight chain (d) Hydrogen wherein OH on carbon 15 is optionally on carbon 16; wherein X=H, OCH3 or OC2H5 when neither C5-C6 or C6-C7 is a double bond and nothing if C5-C6 or C6-C7 is a double bond; wherein R2 is: (a) A 1-8 alkyl optionally containing 1 or 2 unsaturated bond(s) and optionally substituted by methyl, dimethyl or F; (b) A carbocyclic compound of 4-7 carbons having optionally 1 unsaturated bond and having optionally 1 carbon replaced by S or O; (c) Phenyl; (d) Benzyl; (e) -(CH2)m-R4 wherein m is 1-6 and R4 is alkoxy or cycloalkyl; wherein the hydroxyl on carbon 15 is in either the R or S configuration. |
