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US 10,208,036 B2Granted
Process for the preparation of Apixaban and intermediates thereof
AssigneeUnichem Laboratories Ltd
InventorsDhananjay G. 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.
Claims5
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)
2 more elements
Dependencies are inferred from the claim text.