Preparation of bendamustine and its salts
AssigneeDr. Reddy's Laboratories, Inc.
InventorsRajasekhar Kadaboina, Veerender Murki, Venkat Rao Badisa, Nageshwar Gunda
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Abstract
The present application relate to processes for the preparation of bendamustine and its pharmaceutically acceptable salts.
Claims20
A process comprising:
- a) reacting a compound of formula (II):
- wherein R is a C1-C4 alkyl group, with a 2-haloethanol in the presence of an organic base to give a compound of formula (III);
- b) reacting the compound of formula (III) with a chlorinating agent to provide a compound of formula (IV);
- and
- c) hydrolyzing the compound of formula (IV) to give bendamustine hydrochloride.
A process for the purification of bendamustine hydrochloride, comprising:
- a) combining bendamustine hydrochloride, aqueous hydrochloric acid, and acetonitrile;
- b) heating the mixture of step a) to a temperature from about 35° C. to about 65° C.;
- c) cooling the mixture of step b) to a temperature from about 0° C. to about 35° C.;
- and
- d) isolating bendamustine hydrochloride.
A compound of the formula (IIIa):
A process for the preparation of bendamustine hydrochloride, comprising subjecting the compound of the formula (IIIa) to suitable reaction conditions
A compound of the formula (IIa):
A process for the preparation of bendamustine hydrochloride, comprising subjecting the compound of the formula (IIa) to suitable reaction conditions
A compound of the formula (IVa):
A process for the preparation of bendamustine hydrochloride, comprising subjecting the compound of the formula (IVa) to suitable reaction conditions
Bendamustine hydrochloride having purity greater than 99.8% and with less than about 0.1% of each of the compound given in the table below:
- Code
- Structure
- HP1
- HP2
- Impurity A
- Impurity B′
- Formula IV
- wherein R is C1-C4alkyl.
Dependencies are inferred from the claim text.