Shilpa Medicare Limited

Rafiuddin

Vimal Kumar Shrawat

Prashant Purohit

Akshay Kant Chaturvedi

Vinod Kumar Singh

Veereshappa

Karri Papa Rao

The present invention provides process for preparation of crystalline Bortezomib (Ia) as its monohydrate which is designated as crystalline Form-SB and characterized by having water content ranging between 3.5-6.0% w/w; X-ray powder diffraction pattern comprising characteristic 2&#x3b8;&#xb0; peaks selected from the XRPD peak set of 5.6, 7.5, 9.8, 10.2, 11.3, 15.1, 18.0, 20.5, 21.5 and 23.6&#xb1;0.20 2&#x3b8;&#xb0;, wherein peaks at 9.8 and 11.39&#xb1;0.20 2&#x3b8;&#xb0; are un-split and 100% intensity peak is present at 5.6&#xb1;0.20 2&#x3b8;&#xb0;, DSC isotherm comprising the endothermic peaks ranging between 45 to 60&#xb0; C. (Peak-1) and 175 to 185&#xb0; C. (Peak-2) and IR absorption characteristic peaks approximately at 3387 cm, 3304 cm, 2953 cm, 2927 cm, 2868 cm, 1627 cm, 1455 cm, 1400 cm, 1201 cm, 1150 cm, 1020 cm, 747 cmand 702 cmand Raman absorption spectra having characteristic peaks approximately at 3066 cm, 1583 cm, 1528 cm, 1281 cm, 1213 cm, 1035 cm, 1022 cmand 1004 cm. The invention also provides the use of said crystalline Form-SB as active pharmaceutical ingredient in pharmaceutical compositions for the treatment of cancer.

Crystalline bortezomib process

The present invention provide processes for the preparation of N-[4-Cyano-3-(trifluoro methyl)phenyl]-3-[(4-fluorophenyl)sulphonyl]-2-hydroxy-2-methyl propanamide (I). The present application also provides a method of purification of N-[4-Cyano-3-(trifluoro methyl)phenyl]-3-[(4-fluorophenyl)sulphonyl]-2-hydroxy-2-methyl propanamide (I) using ethyl acetate solvent resulting in the product, substantially free from process related impurities A, B, C and D. The crystalline product of the process according to the present invention having an XRDP pattern as per FIG., is useful as an active pharmaceutical and has anti-androgenic activity.

Process for preparing bicalutamide

The present invention provide process of preparation of (2R,3S)&#x2014;N-carboxy-3-phenylisoserine, N-tert-butyl ester, 13-ester with 5(&#x3b2;)-20-epoxy-1,2(&#x3b1;),4,7(&#x3b2;),10(&#x3b2;),13(&#x3b1;)-hexa hydroxy tax-11-en-9-one 4-acetate 2-benzoate or docetaxel and its trihydrate (I) 

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Raichur, India

Rafiuddin