Granted Patent B2

US 8,158,798 · App. 12/258,480 · Granted Apr 17, 2012

Abstract

Claims (16)

1. A process for preparing a substituted quinolone according to Formula I:

wherein:

R 1 is C 1 -C 4 alkyl;

R 2 is C 1 -C 4 alkyl or C 3 -C 6 cycloalkyl;

R 4 and R 5 are each independently selected from a group consisting of amino, C 1 -C 4 alkylamino, protected amino, and C 1 -C 4 alkyl; and

n is 1 or 2;

said process comprising: the step of reacting a compound of Formula II with compound of Formula III in the presence of a suitable base at about 20° C. to about 80° C., followed by hydrolysis:

wherein

R 3 is unsubstituted or substituted C 1 -C 4 acyloxy; and

R 1 , R 2 , R 4 , R 5 , and n are as defined for Formula I above.

2. The process according to claim 1 , wherein R 1 is methyl.

3. The process according to claim 1 , wherein R 2 is cyclopropyl.

4. The process according to claim 1 , wherein R 4 is methyl.

5. The process according to claim 1 , wherein R 5 is amino.

6. The process according to claim 1 , wherein the quinolone of Formula I is:

7. The process according to claim 1 , wherein the compound of Formula II is:

Assignments (9)