| 摘要 |
<p>New prostaglandin analogues are cpds. of formula (I), their salts with organic acid and inorganic bases, and their esters with 1-4C alcohols. In the formula, one of R1 and R2 is H and the other is OH, or R1+R2 is O; R3 is 1-10C alkyl (opt. substd. by 1-5C alkoxy), 3-7C cycloalkyl, or aryl or furyl (opt. substd. by one or more 1-3C alkyl gps.); and R4 is H or 1-10C alkyl. Their activity is more potent and more differentiated than that of the cpds. with OH instead of OCOR4 disclosed in DT 2357953. The influence of esterification is particularly marked in cpds. with hypertensive activity, which are free from undesired smooth muscle side effects. Specific cpds. (I) include 9-keto-5alpha-acetoxy-16,16-dimethyl-18-oxa-prosta-5,13-dienoic acid. In an example, this is prepd. by acetylation of 9-keto-15 alpha-hydroxy-16,16-dimethyl-18-oxa-prosta-5,13-dienoic acid with acetic anhydride in the presence of pyridine.</p> |
