| 摘要 |
<p>1529852 8-Azaprostaglandins LABAZ 11 March 1976 [21 March 1975] 12034/75 Headings C2C and C2P The invention comprises 8-azaprostaglandins of the Formula I wherein R is H, methyl or ethyl and their preparation by standard methods. The following intermediates are also prepared: silver methyl suberate, 1-chloro-2-heptanone, ethyl DL-pyroglutamate DL-6-hydroxymethyl - 2 - pyrrolidinone, and its 2 - tetrahydropyranyl ether; methyl and ethyl 2-hydroxymethyl - 5 - oxo - 1 - pyrrolidineheptanoate and its 2 - tetrahydropyranyl ether; ethyl and methyl 2 - formyl - 5 - oxo - 1 - pyrrolidineheptanoate; methyl and ethyl 2 - (3 - oxo - -trans- 1 - octenyl) - 5 - oxo - 1 - pyrrolidineheptanoate; diethyl (5 - acetoxypentyl)malonate; 7 - bromoheptanoic acid and its methyl and ethyl esters; and ethyl 3-oxooctanoate. (2 - Oxoheptylidene)triphenylphosphorane is prepared by reacting potassium carbonate with (2 - oxoheptyl)triphenylphosphonium chloride obtained by reacting triphenyl phosphine with 1-chloro-2-heptanone. Pharmaceutical compositions contain the 8- azaprostaglandins of Formula I above in association with non-toxic carriers or excipients therefor. The compounds possess similar pharmacological properties to those of PGE.</p> |
