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US 10,377,710 B2Granted
Process for the preparation of considerably pure Silodosin
AssigneeMankind Pharma Ltd.
InventorsKuldeep Singh Gangwar, Anil Kumar, Bhuwan Bhashkar
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Abstract
The present invention relates to a novel, improved, commercially viable and industrially advantageous process for the preparation of Silodosin of Formula (I), its pharmaceutically acceptable salts or solvates thereof. The invention relates to the preparation of considerably pure Silodosin with high yield.
Claims11
A process for the preparation of Silodosin represented by Formula I;
- wherein the process comprises the steps of:
- a) condensing chiral compound represented by Formula (III)
- wherein, Bz represents to Benzoyl group with compound represented by Formula (IV)
- wherein, Ms represents to Methanesulfonyl group in presence of a base and a phase transfer catalyst in an organic solvent to give intermediate represented by Formula (V)
- wherein, n is an integer of 1 and 2;
- b) without purification converting compound of Formula (V) to de-protected compound represented by Formula (IX) in an organic solvent;
- wherein, n is as defined above;
- c) without purification converting compound of Formula (IX) to a compound represented by Formula (X)
- wherein n is as defined above;
- d) subjecting compound of Formula (X) to purification by converting to an oxalate salt in presence of isopropyl alcohol for removal of N,N-dialkyl impurity represented by Formula (IIc);
- e) hydrolysis of the oxalate salt formed in step d) to obtain Silodosin of Formula (I), wherein said Silodosin has N,N-dialkyl impurity in an amount less than 0.03%.
8 more elements
A process for purification of crude Silodosin of Formula (X);
- wherein, n is an integer of 1 and 2;
- comprising the steps of:
- a) converting crude Silodosin of Formula (X) to its oxalate salt in presence of isopropyl alcohol for removal of N,N-dialkyl impurity of Formula (IIc);
- b) hydrolysis of the said oxalate salt to get pure Silodosin of Formula (I)
- wherein said Silodosin has N,N-dialkyl impurity in an amount less than 0.03%.
2 more elements
Dependencies are inferred from the claim text.