Abstract:
Methods and novel intermediates for the preparation of acyclic nucleoside derivatives of formula (I) where one of R1 and R2 is an amino acid acyl group and the other of R1 and R2 is a -C(O)C3-C21 saturated or monounsaturated, optionally substituted alkyl and R3 is OH or H; or a pharmaceutically acceptable salt thereof.
Abstract:
THERE IS DISCLOSED A CRYSTALLINE POLYMORPH AND A GREATER THAN 90% PURE CRYSTALLINE POLYMORPH OF (2S, 3S, 5S)-5-(N-(N-((-METHYL-N-((2-ISOPROPYL-4-THIAZOLYL)ME-THYL)AMINO)CARBONYL)-L-VALINYL)AMINO)-2-(N-((5-THIAZOLYL)METHOXYCARBONYL)AMINO)-1, 6-DIPHENYL-3-HYDROXYHEXANE. IT HAS CHARACTERISTIC PEAKS IN THE POWDER X-RAY DIFFRACTION PATTERN AT VALUES OF TWO THETA OF 8.67°± 0.1, 9.88°±0.1°, 16.11° ± 0.1°, 16.70° ± 0.1°, 17.36° ± 0.1°, 17.78° ± 0.1°, 18.40° ± 0.1°, 18.93° ± 0.1° 20.07° ± 0.1°, 20.65° ± 0.1°, 21.71° ± 0.1° AND 25.38° ± 0.1°. A PROCESS FOR THE PREPARATION OF THE GREATER THAN 90% PURE CRYSTALLINE POLYMORPH IS ALSO DISCLOSED.
Abstract:
SUBSTANTIALLY PURE AMORPHOUS RITONAVIR IS DISCLOSED. ALSO DISCLOSED A PROCESS FOR THE PREPARATION OF SUBSTANTIALLY PURE RITANOVIR CRYSTALLINE POLYMORPH FORM I COMPRISING ADDING A SOLUTION OF RITONAVIR TO A SLURRY OF SEED CRYSTALS OF RITONAVIR CRYSTALLINE POLYMORPH FORM I IN AN ANTI-SOLVENT.