Process for the preparation of apixaban and intermediates thereof
AssigneeUnichem Laboratories Ltd
InventorsDhananjay D. Sathe, Arijit Das, Yashwant Surve, Ramdas N. Ahire
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Abstract
The present invention refers to novel process for the preparation of Apixaban. Further, the invention also related to a process for the preparation of intermediate of Apixaban from very basic and cheap row material i.e. Aniline which is widely commercially available. The present invention provides process for preparation of Apixaban using a different sequence of synthetic steps and does not involve use of Ullmann reaction.
Claims10
A process for preparation of amino-morpholine compound of the formula (17) comprising steps of:
- a. reacting a compound of formula (10) with chlorinating agent in presence of non-halogenated solvent to obtain compound of formula (11);
- b. reacting compound of formula (11) with morpholine optionally in presence of solvent to obtain nitro-morpholine compound of formula (16);
- c. optionally isolating and purifying the nitro-morpholine compound of formula (16);
- and
- d. reducing nitro-morpholine compound of formula (16) in presence of a hydrazine hydrate with catalytic amount of Raney Nickel to obtain amino-morpholine compound of formula (17).
A process for preparation of lactam compound of formula (18) comprising steps of;
- a. reacting amino-morpholine compound of formula (17) with compound of formula (22) in presence of inorganic base or aqueous solution of inorganic base or absence of any base optionally in presence of phase transfer catalyst to obtain amide-compound of formula (23), wherein X is leaving group;
- b. optionally isolating the amide-compound of formula (23);
- and
- c. cyclizing amide-compound of formula (23) in presence of inorganic base or aqueous solution of inorganic base optionally in presence of phase transfer catalyst to obtain a lactam compound of formula (18).
Dependencies are inferred from the claim text.