Crystal comprising (2R)-2-propyloctanoic acid and amine
AssigneeOno Pharmaceutical Co., Ltd.
InventorsTomoyuki Hasegawa, Yasufumi Kawanaka, Eiji Kasamatsu
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Abstract
According to the present invention, crystals comprising (2R)-2-propyloctanoic acid and an amine, which can be used as bulk drugs for safely orally administrable solid preparations with keeping the pharmacological effect, are provided. Among these crystals, the crystal with dibenzylamine per se is particularly useful as bulk drug for pharmaceuticals and can be used as an intermediate to produce (2R)-2-propyloctanoic acid having an optical purity of more than 99.5% e.e. which has not been obtained.
Claims1
A process for producing (2R)-2-propyloctanoic acid having an optical purity of 99.5% e.e. or more, which comprises:
- dissolving (2R)-2-propyloctanoic acid having an optical purity of 70% e.e. or more and dibenzylamine in a solvent to give a solution;
- repeating the following steps (1)-(3) 0 to 3 times:
- (1) preferentially crystallizing a crystal comprising the (2R)-2-propyloctanoic acid with dibenzylamine from the solution;
- (2) separating and collecting the precipitated crystal;
- (3) dissolving the crystal in a solvent to give a solution;
- preferentially crystallizing a crystal comprising the (2R)-2-propyloctanoic acid with dibenzylamine from the solution;
- and
- separating, collecting, back-extracting and extracting the precipitated crystal to give a free (2R)-2-propyloctanoic acid.
Dependencies are inferred from the claim text.