Biohaven Therapeutics Ltd.

Hangzhou Highlightll Pharmaceutical Co., Ltd.

Haihui Liu

Laibao Wang

Congxin Liang

A method for synthesizing a compound 2-[(2R,5S)-5-[2-methylfuro[3,2-b]imidazo[4,5-d]pyridin-1-yl]tetrahydropyran-2-yl]acetonitr ile as a selective JAK1/TYK2 kinase inhibitor. The compound is prepared by taking 7-chloro-6-nitrofuro[3,2-b]pyridine as the starting material, and by nucleophilic substitution, palladium on carbon reduction and cyclization reactions. The present synthesis method has mild reaction conditions, high product yield and high purity, and is suitable for industrial production. A crystal form of the compound, crystal forms of the salts thereof and preparation methods thereof. The crystal form of the compound and the crystal forms of the salts thereof have good physical and chemical properties and are suitable for drug development.

Method for synthesizing furoimidazopyridine compound, polymorphic substance and polymorphic substance of salt

Provided is a method for synthesizing a compound 2-[(2R,5S)-5-[2-[(R)-1-hydroxyethyl]furo[3,2-b]imidazo[4,5-d]pyridin-1-yl]tetrahydropyran-2-yl]acetonitrile as a selective JAK1/TYK2 kinase inhibitor. The compound is prepared by nucleophilic substitution, palladium on carbon reduction, and cyclization reaction using 7-chloro-6-nitrofuro[3,2-b]pyridine as a starting material. The synthesis method has mild reaction conditions, high product yield, and high purity, and is suitable for industrial production. Further provided are a crystal form of the compound, crystal forma of its salts, and their preparation methods. The crystal form of the compound and the crystal forms of its salts have good physical and chemical properties and are suitable for drug development.

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Shanghai, China

Haihui Liu