Ptc Therapeutics, Inc.

Sumitomo Pharma Co., Ltd.

Shinjiro Tsuyumine

Yoko Takahashi

Hiroto Tatamidani

Kiyoto Sawamura

Kiichi Kuroda

The present invention provides a method for chiral resolution of Trolox. The present disclosure relates to a method for producing a solid salt of a compound of formula I, wherein an amide-based solvent is added to a sample, which contains a compound of formula I, while being assumed to contain a compound of formula II, in the presence of an optical resolution agent:

Optically resolved Trolox intermediate and method for producing same

The present invention provides a method in which when using (+)-dibenzoyl-D-tartaric acid to optically divide (±)-1-methyl-4-(2,4,6-trimethoxyphenyl)-3-piperidinone, an ether-based solvent is added and an extremely high yield of (R)-1-methyl-4-(2,4,6-trimethoxyphenyl)-3-piperidinone (+)-dibenzoyl-D-tartrate is thereby obtained, a slurry thereof is treated with a base, a 'three-dimensionally bulky reducing agent' is subsequently used, and cis-(−)-flocinopiperidol is thereby produced with surprisingly high selectivity.

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Osaka, Japan

Shinjiro Tsuyumine