Takeda Pharmaceutical Company Limited

Yasuhiro Sawai

Naotaka Sawada

Yoichi Kawabata

Kazuaki Kanno

Mitsuo Yamamoto

Mitsuhisa Yamano

Masato Kitayama

Masahiro Mizuno

Kentaro Iwata

Miyuki Hohokabe

Koya Kimoto

The present invention provides a cocrystal of (S)-3-(1-((1-acryloylpyrrolidin-3-yl)oxy)isoquinolin-3-yl)-1H-1,2,4-triazol-5(4H)-one and an organic acid capable of forming a cocrystal with the compound.

Cocrystal, production method thereof, and medicament containing cocrystal

The present invention provides an advantageous production method of an imidazole derivative, which is suitable for industrial production. Compound (VI) is produced by reacting compound (I) with a Grignard reagent or a magnesium reagent, and a lithium reagent, and then reacting the resulting compound with compound (V).

Production method of imidazole derivatives

Disclosed is a vinamidinium salt represented by the formula (I): [wherein Rrepresents a hydrogen atom, a halogen atom, an optionally substituted hydrocarbon group or the like; Rand Rare the same or different and each represents a lower alkyl group, or alternatively Rand Rmay combine together to form a ring; Rand Rare the same or different and each represents a lower alkyl group, or alternatively Rand Rmay combine together to form a ring; X and Y are the same or different and each represents a bromine atom or a chlorine atom; n represents a number of not less than 2; and m represents 0 or n], and methods for synthesizing a heterocyclic ring compound using the salt.

Stable vinamidinium salt and nitrogen-containing heterocyclic ring synthesis using the same

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Osaka, Japan

Yasuhiro Sawai