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N-(2-(6-fluoro-1H-indol-3-yl)ethyl-3-(2,2,3,3-tetrafluoropropoxy) benzylamine phosphate salt

IP.com Disclosure Number: IPCOM000247734D
Publication Date: 2016-Oct-02
Document File: 2 page(s) / 208K

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N-(2-(6-fluoro-1H-indol-3-yl)ethyl-3-(2,2,3,3-tetrafluoropropoxy)

benzylamine Phosphate salt

Provided herein is a process for preparing crystalline form 1 of N-(2-(6-fluoro-1H-indol-3- yl)ethyl-3-(2,2,3,3-tetrafluoropropoxy)benzylamine Phosphate salt. Crystalline form 1 of N-(2-(6-fluoro-1H-indol-3-yl)ethyl-3-(2,2,3,3-tetrafluoropropoxy)benzylamine Phosphate salt can be prepared according to examples 1 or 2.

EXAMPLE-1

N-(2-(6-fluoro-1H-indol-3-yl)ethyl-3-(2,2,3,3-tetrafluoropropoxy)benzylamine HCl Form-I
0.5 gm was added to 50ml of 0.2 molar monobasic potassium phosphate solution in water which was adjusted to pH 6.8 with 0.2 molar NaOH at 20-25ºC and the obtained slurry was stirred for 18 hours. The obtained solid was filtered under vacuum and kept under suction for about 20 minutes to obtain solid was about 0.4 gm.

EXAMPLE-2

N-(2-(6-fluoro-1H-indol-3-yl)ethyl-3-(2,2,3,3-tetrafluoropropoxy)benzylamine HCl Form-I
0.5 gm was added to 50ml of 0.2 molar monobasic potassium phosphate solution in water which was adjusted to pH 6.8 with 0.2 molar NaOH at 20-25ºC and the obtained slurry was stirred for 56 hours. The obtained solid was filtered under vacuum and kept under suction for about 20 minutes to obtain solid was about 0.45 gm.

Figure 1 shows a powder X-ray diffraction pattern ("powder XRD" or "PXRD") of Form-1 of N-(2-(6-fluoro-1H-indol-3-yl)ethyl-3-(2,2,3,3-tetrafluoropropoxy)benzylamine Phosphate salt. Characteristic peaks are at 8.0; 11.8; 13.4; 14.1; 14.8; 1...