Succinic Acid → Batefenterol Succinate

Participants

Reaction Steps

Biphenyl-2-ylcarbamic acid 1-[2-(2-chloro-4-{[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethylamino]methyl}-5-methoxyphenylcarbamoyl)-ethyl]piperidin-4-yl ester (2 g) was dissolved in methanol (16 ml) at ˜70° C., over a period of 1 h. After a further 1 h, succinic acid (335 mg) in methanol (4 ml) was added and this was left to temperature cycle between 0° C. and 40° C. over 2 days. The resulting solid was isolated by filtration, washed with methanol, dried on filter paper and then dried at 40° C. in a vacuum oven overnight, to provide the title compound as a crystalline solid (979 mg). This was confirmed by DSC to be Form 2.

Provenance & Evidence