反应详情

Perindopril (I) prepared exactly as per the method described in our pending PCT Application No. PCT/IN03/00042, dated Feb. 28, 2003 and as per the chemistry summarized in Scheme-II and as mentioned hereinbefore in Section 1 (b) was suspended in 2,2-dimethoxypropane (instead of ethyl acetate) to which was gradually tertiary-butylamine. The mixture was heated to reflux till a clear solution was obtained and filtered hot to remove any suspended particles. Thereafter, the solution was cooled to 20° C. to 30° C., and then further cooled to 0° C. to 15° C., maintained at the same temperature for 30 minutes to 1 hour and finally the crystallized solid was filtered and dried at 40-45° C. under vacuum for 5-6 hours to give crystalline perindopril erbumine (IU), exhibiting IR spectra values and, DSC thermogram summarized hereinbelow

1. temperatureThe mixture was heated
2. temperatureto reflux till a clear solution
3. customwas obtained
4. filtrationfiltered hot
5. customto remove any suspended particles
6. temperatureThereafter, the solution was cooled to 20° C. to 30° C.
7. temperaturefurther cooled to 0° C. to 15° C.
8. temperaturemaintained at the same temperature for 30 minutes to 1 hour
9. filtrationfinally the crystallized solid was filtered
10. customdried at 40-45° C. under vacuum for 5-6 hours