The present invention provides substantially pure desloratadine having an
HPLC purity greater than 99.5% and having an absorbance less than 0.15 Au
at 420 nm for a 5% w/v solution in methanol, which does not show a peak
for an impurity at a relative retention time in the range from about 0.85
to about 0.99 (relative to desloratadine appearing at a retention time of
25.+-.5 minutes), which is greater than the discard limit set at less
than 0.025% of the total area, when tested according to an HPLC method
performed using a Hypersil BDS C.sub.8 column (15 cm.times.4.6 mm, 5
.mu.m particle size) with the following parameters:
TABLE-US-00001
Mobile phase: Buffer solution having a pH of about 3, methanol and
acetonitrile in a volume ratio of 8:1:1.
Injection volume: 20 .mu.l
Flow rate: 1.5 ml/minute
Run time: 75 minutes.
Discard limit: Set at less than 0.025% of total area
The present invention also provides a process for the preparation of
substantially pure desloratadine by the process comprising acidic
hydrolysis of a compound of formula 3 where R is selected from COR.sub.1,
COOR.sub.1 wherein R.sub.1 is selected from branched or linear alkyl (1-6
C), cycloalkyl, alkenyl, alkynyl, aryl, aralkyl and their substituted
analogs; and their substituted analogs with a strong organic acid or a
mineral acid. ##STR00001##