METHOD FOR PREPARING TOLIMIDONE ON LARGE SCALE

WIPO Patent Application WO/2019/139185

A1

The present disclosure relates to a method for preparing tolimidone on large scale with maintaining high purity and uniform particle size distribution, and more specifically, a method suitable for preparing tolimidone on industrially large scale by using tetrabutyl ammonium bromide catalyst and recrystallization in ethanol, which can prepare highly pure tolimidone in a time shorter than prior arts while maintaining water content and particle size distribution constantly.

LEE KWANG OK (KR)
LEE KYUNG HWA (KR)
JEONG EUN JU (KR)

PCT/KR2018/000530

July 18, 2019

January 11, 2018

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BUKWANG PHARMACEUTICAL CO LTD (KR)

C07D239/52; A61K31/513; A61P3/10

WO2013090319A2

2013-06-20

US3922345A	1975-11-25
KR20160065496A	2016-06-09
KR101827744B1	2018-02-09
US3922345A	1975-11-25

LIPINSKI, C. A. ET AL.: "Bronchodilator and antiulcer phenoxypyrimidinones", JOURNAL OF MEDICINAL CHEMISTRY, vol. 23, no. 9, 1980, pages 1026 - 1031, XP002201971, doi:10.1021/jm00183a012
THE JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, vol. 342, no. 1, 2012, pages 23 - 32
JOURNAL OF MEDICINAL CHEMISTRY, vol. 23, 1980, pages 1026 - 1031
JOURNAL OF PHARMACEUTICAL SCIENCES, vol. 99, no. 1, 2010, pages 51 - 75
INTERNATIONAL JOURNAL OF PHARMACEUTICS, vol. 122, no. 1-2, 1995, pages 35 - 47
See also references of EP 3737669A4

HANSUNG INTELLECTUAL PROPERTY (KR)

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