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AssigneeHetero Research Foundation
InventorsBandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Rapolu Raji Reddy, Bandi Vamsi Krishna, Adulla Venkat Narsimha Reddy
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4-[[6-chloro-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3,5-dimethyl-benzonitrile is a key intermediate for the preparation of etravirine. The present invention provides a process for preparation of 4-[[6-chloro-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3,5-dimethylbenzonitrile. The present invention also provides a novel process for the preparation of etravirine crystalline form I. The present invention further provides novel crystalline forms of etravirine, processes for their preparation and pharmaceutical compositions comprising them.
A process for the preparation of 4-[[6-chloro-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3,5-dimethylbenzonitrile of formula I:
A process for the preparation of etravirine crystalline form I, which comprises:
A etravirine crystalline form II which is characterized by peaks in the powder x-ray diffraction spectrum having 2θ angle positions at about 11.1, 12.2, 13.1, 13.8, 18.1, 18.4, 19.8, 21.3, 22.7, 22.9, 24.5 and 27.2±0.2 degrees.
A etravirine crystalline form II, characterized by an x-ray powder diffractogram as shown in FIG. 2.
A etravirine crystalline form III which is characterized by peaks in the powder x-ray diffraction spectrum having 2θ angle positions at about 6.0, 8.7, 9.1, 11.2, 12.1, 13.7, 18.1, 19.8, 22.9, 24.4, 25.3 and 27.3±0.2 degrees.
A etravirine crystalline form III, characterized by an x-ray powder diffractogram as shown in FIG. 3.
A pharmaceutical composition comprising novel crystalline forms of etravirine selected from crystalline form II and crystalline form III or a mixture thereof;
Dependencies are inferred from the claim text.