Browse Prior Art Database

Intermediates of (S)-N-[2-(1,6,7,8-tetrahydro-2H-indeno-[5,4-b]furan-8-yl)ethyl]propionamide

IP.com Disclosure Number: IPCOM000168326D
Publication Date: 2008-Mar-06
Document File: 3 page(s) / 141K

Publishing Venue

The IP.com Prior Art Database

This text was extracted from a PDF file.
At least one non-text object (such as an image or picture) has been suppressed.
This is the abbreviated version, containing approximately 100% of the total text.

Page 1 of 3

Impurity Profile for ROZEREMTM Tablets

    (S)-N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl propionamide having the following chemical structure:

O N H

is a melatonin receptor agonist with both high affinity for melatonin MT1 and MT2 receptors and selectivity over the MT3 receptor. This API has been formulated as ROZEREMTM tablet.

    In order to analyze impurities, an 8mg "ROZEREM" tablet was diluted in 5ml of H20: Acetonitrile, and then was filtered and injected into an Xterra® column 150x4.6mm. Chromatographic analysis was with wavelength set to 288nm. The eluent contained Acetonitrile and KH2PO4 at pH 3.0 as buffer, and the gradient was operated at
1.5mL/min. The injection volume was 10µl.

The following results were obtained:

 RT 1.51 5.06 6.59 10.46 12.77 13.93 17.89 20.07 21.12 24.08 RRT 0.11 0.36 0.47 0.75 0.92 1.00 1.28 1.44 1.52 1.73 % 0.04 0.06 0.02 0.03 0.06 99.61 0.05 0.02 0.04 0.07

O

I

Page 2 of 3

    In another analysis impurities, another 8mg "ROZEREM" tablet was diluted in 5ml of Heptane: Ethanol, and then was filtered and injected into an chiral column 250X4.6mm. Chromatographic analysis was with wavelength set to 288nm. The eluent contained Heptane: Ethanol at. and the gradient was operated at 1.0ml/min. The injection volume was 10µl.

The following result and chromatogram was obtained:

% R - RML: N.D.

[This page contains 1...