ANALOGIFORFARANDE FOR FRAMSTELLNING AV NYA, ANTIBAKTERIELLT AKTIVA DERIVAT AV AMIDINOPENICILLANSYRA

摘要

1427139 Penicillanic acids ASTRA LAKEMEDAL AB 12 March 1973 [13 March 1972] 11689/72 Heading C2C [Also in Division A5] Novel penicillanic acid derivatives of Formula I and therapeutically acceptable salts thereof, wherein R1 and R2, which may be the same or different, are each a C 1 -C 10 alkyl, alkenyl or alkynyl group, a C 3 -C 7 cycloalkyl group or a C 4 -C 10 cycloalkylalkyl group or wherein R1 and R2 together with the adjacent nitrogen atom form a heterocyclic ring; R3 is or wherein R4 is an alkyl group of 1 to 8 carbon atoms, or a phenyl group which may be unsubstituted or substituted by one or more amino groups, halogen or C 1 -C 4 alkoxy groups; and R5 is H, or -C 2 H 5 , are prepared (a) by reacting a reactive derivative of a compound of formula wherein R1 and R2 are as defined above and R6 is O or S, with a compound of Formula IV wherein R 3 is as defined above, or (b) by reacting a compound of formula wherein R1 and R2 are as defined above and R7 is a C 1 -C 6 alkyl group, with a compound of Formula IV, or (c) by reacting a compound of formula wherein R1 and R2 are as defined above with a compound of formula Y1R3 (VIII), wherein Y1 is halogen or an equivalent group which will react to form an ester linkage, and R3 is as defined above. Pharmaceutical compositions having antibiotic activity comprise a compound of Formula I or a pharmaceutically acceptable salt thereof together with a pharmaceutically acceptable diluent.