Hydrochloric Acid → Afuresertib Hydrochloride

Participants

Reaction Steps

The hydrochloride salt of N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide prepared generally as described in Example 96 of International Application No. PCT/US2008/053269, having an International Filing date of Feb. 7, 2008, and having International Publication Number WO/2008/098104 and an International Publication Date of Aug. 14, 2008, which generally states that the free base compound, N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide, is treated with 4M HCl in dioxane and after 5 min, the solution is concentrated and dried under vacuum to afford N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide hydrochloride, yielded an amorphous solid as indicated by the Powder X-Ray Diffraction (PXRD) pattern depicted in FIG. 3.

Provenance & Evidence