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A CRYSTALLINE FORM OF(S)-2-(2-CHLOROPHENYL)-2-HYDROXYETHYL CARBAMATE

IP.com Disclosure Number: IPCOM000200979D
Publication Date: 2010-Nov-02
Document File: 3 page(s) / 85K

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A CRYSTALLINE FORM OF(S)-2-(2-CHLOROPHENYL)-2-HYDROXYETHYL

CARBAMATE

    (S)-2-(2-chlorophenyl)-2-hydroxyethyl carbamate ("referred as CRS"), having the following formula;

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is an NMDA antagonist for the treatment of epilepsy. Crystalline form of CRS was found and is described herein below.

Crystalline form of CRS form C1 maybe characterized by data selected from a powder XRD pattern with peaks at 11.2, 12.2, 14.0, 16.6, 17.4, 18.4, 19.2, 20.0, 21.0,
21.7, 22.3, 22.8, 23.3, 24.5, 25.1, 25.7 and 26.3 degrees two theta ± 0.2 degrees two- theta; a PXRD pattern depicted in Figure 1; a PXRD pattern depicted in Figure 2; and combination thereof.

Figure 1: An X-ray powder diffractogram of a mixture of CRS form C1 and form A

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Figure 2: An X-ray powder diffractogram of CRS form C1.

02.0 6.0 10.0 14.0 18.0 22.0 26.0 30.0 34.0 38.0


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* The peak at 28.5 corresponds to Si

X-ray powder diffraction:

    The X-ray powder diffraction of CRS form C1 was performed on an ARL X- ray powder diffractometer model X'TRA-019, with a Peltier detector. Copper Kα1

radiation (λ=1.5418 Å) was used. The sample holder was a round standard aluminum sample holder with round zero background plate (quartz or silicon).The scanning parameters were: range: 2-40 degrees two-theta; scan mode: continuous scan; step size: 0.05o; and scan rate: 3 degrees/minute.

    The peak positions were determined by using silicon powder as internal standard in an admixture with the sample measured. The position of the silicon (111) peak was corrected to be 28.45 degrees two theta. The positions of the peaks were corrected respectively (no cor...