Takeda Pharmaceutical Company Limited

Aetas Pharma Co., Ltd.

Dot Therapeutics-1, Inc.

Day One Biopharmaceuticals, Inc.

Sayuri Hirano

Masatoshi Yamada

Yoshiyuki Takeda

Masato Kitayama

Jun-ichi Kawakami

Koji Nakamoto

Motoki Ikeuchi

Mitsuhisa Yamano

Ryoji Tsuruoka

The present invention addresses the problem of providing an efficient asymmetric synthesis method for an optically active 1,4-benzothiazepine-1-oxide derivative. [Solution] According to the present invention, an optically active 1,4-benzothiazepine-1-oxide derivative is efficiently produced by reacting a 1,4-benzothiazepine derivative or a salt thereof with a reagent containing a titanium compound, a chiral diol compound and water, and an oxidant in a solvent.

Method for producing optically active 1, 4-benzothiazepine-1-oxide derivative

The aim of the present invention is to provide a method capable of producing an optically active pyrimidinamide derivative on an industrial scale. Compound (I) or a salt thereof is subjected to an asymmetric reduction reaction, the obtained compound (II) or a salt thereof is subjected to a deprotection reaction, and the obtained compound (III) or a salt thereof is reacted with compound (VI) or a salt thereof to obtain compound (V) or a salt thereof.

Method for producing optically active compound

The aim of the present invention is to provide a method capable of producing an optically active pyrimidinamide derivative on an industrial scale. Compound (I) or a salt thereof is subjected to an asymmetric reduction reaction, the obtained compound (II) or a salt thereof is subjected to a deprotection reaction, and the obtained compound (III) or a salt thereof is reacted with compound (VI) or a salt thereof to obtain compound (V) or a salt thereof. wherein each symbol is as defined in the specification.

The present invention provides a method of efficiently producing an optically active 6-(3-aminopiperidin-1-yl)-2,4-dioxo -1,2,3,4-tetrahydropyrimidine derivative. The optically active piperidine-3-carboxamide or a derivative thereof, which is obtained by subjecting 1,4,5,6-tetrahydropyridine -3-carboxamide or a derivative thereof to an asymmetric reduction in the presence of a catalyst, is used as an intermediate.

Process for producing heterocyclic compound

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Osaka, Japan

Sayuri Hirano