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Amorphous N-(2-(4-(4-fluorobenzylcarbamoyl) -5-hydroxy-1-methyl-6-oxo-1, 6-dihydropyrimidin-2-yl)propan-2-yl) -5-methyl-1,3,4-oxadiazole-2- carboxamide potassium salt

IP.com Disclosure Number: IPCOM000194495D
Publication Date: 2010-Mar-28
Document File: 2 page(s) / 67K

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The IP.com Prior Art Database

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Amorphous N-(2-(4-(4-fluorobenzylcarbamoyl) -5-hydroxy-1-methyl-6-oxo-1, 6- dihydropyrimidin-2-yl)propan-2-yl) -5-methyl-1,3,4-oxadiazole-2- carboxamide potassium salt
N-(2-(4-(4-fluorobenzylcarbamoyl) -5-hydroxy-1-methyl-6-oxo-1, 6-dihydropyrimidin- 2-yl)propan-2-yl) -5-methyl-1,3,4-oxadiazole-2- carboxamide potassium salt is known as RLT-
K. RLT-K has the molecular formula: C20H20FKN6O5, a molecular weight of 482.51gr/mol and the following chemical structure:

O

OK

F

N

N

N

H

N

O

H

N

O

N

O

RLT-K is an antiretroviral drug used to treat HIV infection.

    Amorphous RLT-K was found and described herein. Amorphous RLT-K may be characterized by X-ray powder diffraction ("XRPD") pattern as depicted in figure 1.

Figure 1: XRPD of amorphous RLT-K * The peak at 28.5 corresponds to Si.

Absorbance Units

5001000150020002500

5 10 15 20 25 30 35 40

    The x-ray powder diffraction was performed on a Scintag X-ray powder diffractometer model X'TRA, with a Cu-tube solid-state detector, round standard aluminum sample holder with round zero background quartz plate with cavity of 25 (diameter)*0.5 (dept.) mm. Copper

1

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1 radiation (λ=1.5418 Å) was used. The scanning parameters were: range: 2-40 degrees two- theta; scan mode: continuous scan; step size: 0.05 deg.; and scan rate: 3 deg/min.

    Example 1: Preparation of amorphous N-(2-(4-(4-fluorobenzylcarbamoyl) -5- hydroxy-1-methyl-6-oxo-1, 6-dihydropyrimidin-2-yl)propan-2-yl) -5-methyl-1,3,4- oxadiazole-2- carboxamide potassium...