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US 10,118,924 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.
Claims10
A process for preparation of compound of formula (21) comprising steps of;
- a. reacting aniline with a compound of formula (22) in presence of an inorganic base or aqueous solution of inorganic base or absence of any base optionally in presence of a phase transfer catalyst to obtain a compound of formula (24), wherein X is a leaving group;
- b. optionally isolating the compound of formula (24);
- c. cyclizing the compound of formula (24) in presence of an inorganic base or aqueous solution of the inorganic base optionally in presence of a phase transfer catalyst to obtain compound of formula (21)
A process for preparation of compound of formula (10) comprising steps of;
- a. reacting aniline with a compound of formula (22) in presence of an inorganic base or aqueous solution of the inorganic base or absence of any base optionally in presence of a phase transfer catalyst to obtain a compound of formula (24), wherein X is a leaving group;
- b. optionally isolating the compound of formula (24);
- c. cyclizing the compound of formula (24) in presence of an inorganic base or aqueous solution of the inorganic base optionally in presence of a phase transfer catalyst to obtain a compound of formula (21);
- d. optionally isolating compound of formula (21);
- e. nitrating the compound of formula (21) with nitric acid in sulphuric acid or acetic acid to obtain compound of formula (10)
2 more elements
Dependencies are inferred from the claim text.