Process for preparation of Bicalutamide
A process for preparation of Bicalutamide of formula (I), comprising oxidation of compound of formula (II), with potassium permanganate in presence of water or a mixture of water and water miscible solvent and isolating Bicalutamide of formula (I) thereof.
1. A process for preparation of Bicalutamide of formula (I),
comprising:
oxidizing of compound of formula (II),
with potassium permanganate in presence of water or with potassium permanganate in the presence of a mixture of water and water miscible solvent; and
isolating Bicalutamide of formula (I).
2. A process according to claim 1 , wherein oxidizing is carried out at a temperature of 25-60° C.
3. A process according to claim 1 , wherein oxidizing is carried out at a temperature of 25-45° C.
4. A process according to claim 1 , wherein the water miscible solvent is selected from a nitrile, a ketone and an aliphatic acid.
5. A process according to claim 4 , wherein the nitrile is selected from acetonitrile, propionitrile and benzonitrile.
6. A process according to claim 4 , wherein the ketone is selected from acetone, methyl isobutyl ketone, methyl ethyl ketone and cyclohexanone.
7. A process according to claim 4 , wherein the aliphatic acid is selected from acetic acid, propionic acid and butyric acid.
8. A process according to claim 1 , wherein the water miscible organic solvent comprises acetonitrile.
9. A process according to claim 1 , wherein the water miscible organic solvent comprises acetone.
10. A process according to claim 1 , wherein the water miscible organic solvent comprises acetic acid.
11. A process according to claim 1 , wherein the ratio of water to the water miscible organic solvent is between 1:1 and 1:4.
12. A process according to claim 1 , wherein the ratio of water to the water miscible organic solvent is between 1:1 and 1:2.
13. A process according to claim 1 , wherein potassium permanganate is in molar proportions of 1 to 3 equivalent per mole of compound of formula (II).
14. A process according to claim 1 , wherein potassium permanganate is in molar proportions of 2 to 3 equivalent per mole of compound of formula (II).
15. A process according to claim 1 , wherein isolated Bicalutamide of formula (I) employs acetonitrile.
16. A process according to claim 15 , further comprising crystallizing Bicalutamide of formula (I) from a mixture of ethyl acetate and petroleum ether.
17. A process for preparation of Bicalutamide of formula (I)
comprising:
oxidizing a compound of formula (II),
with potassium permanganate in the presence of water or with potassium permanganate in the presence of a mixture of water and water miscible solvent; wherein the water miscible solvent comprises acetonitrile, propionitrile, benzonitrile, acetone, methyl isobutyl ketone, methyl ethyl ketone, cyclohexanone, acetic acid, propionic acid, or butyric acid; and
isolating Bicalutamide of formula (I).
18. The process of claim 17 , wherein the water miscible organic solvent comprises acetonitrile, acetone, or acetic acid.
19. The process of claim 18 , wherein the water miscible organic solvent comprises acetonitrile.
20. The process of claim 17 , wherein the ratio of water to the water miscible organic solvent is 1:1 to 1:4.
21. The process of claim 17 , wherein potassium permanganate is in molar proportions of 1 to 3 equivalent per mole of compound of formula (II).
22. The process of claim 17 , wherein isolating employs acetonitrile.
23. The process of claim 22 , further comprising crystallizing Bicalutamide of formula (I) from a mixture of ethyl acetate and petroleum ether.