Yuhan Corporation

Kyoung-Chan Kwon

Hyun Ju

Ja-Heouk Khoo

Chun-Ho Lee

Ji-Hye Choi

Sang-Ho Oh

Tai-Au Lee

Doo-Byung Lee

Kyu-Jung Wang

Hong-Bae Kim

Chang-Hoe Ku

Sung-Hee Cho

Kyeong-Sill Lee

Sang-Won Kim

Su-Young Lee

Ik-Su Jo

Hyo-Ick Hwang

Provided are a process for preparing (3R,4R)-1-benzyl-N,4-dimethylpiperidin-3-amine or a salt thereof, which is an intermediate useful for the preparation of tofacitinib, an intermediate used in the process, i.e., isopropanol solvate of methyl ((3R,4R)-1-benzyl-4-methylpiperidin-3-yl)carbamate dibenzoyl-L-tartrate, an intermediate, having excellent stability, useful for the preparation of tofacitinib, i.e., (3R,4R)-1-benzyl-N,4-dimethylpiperidin-3-amine acetate, and a process for preparing tofacitinib or a pharmaceutically acceptable salt thereof.

Processes for preparing (3R,4R)-1-benzyl-N,4-dimethylpiperidin-3-amine or a salt thereof and processes for preparing tofacitinib using the same

The present invention relates to a process for preparing 2-methyl-2'-phenylpropionic acid derivatives showing antihistamine activity in more simplified way, intermediate compounds and their preparation processes used therefor. According to the present invention, pharmaceutically useful 2-methyl-2&#x2032;-phenylpropionic acid derivatives can be prepared with high yield and purity on industrial scale.

Process for preparation of 2-methyl-2'-phenylpropionic acid derivatives and novel intermediate compounds

The present invention relates to a process for preparing 2-methyl-2'-phenylpropionic acid derivatives showing antihistamine activity in more simplified way, intermediate compounds and their preparation processes used therefore. According to the present invention, pharmaceutically useful 2-methyl-2&#x2032;-phenylpropionic acid derivatives can be prepared with high yield and purity on industrial scale.

Process for preparation of 2-methyl-2' phenylpropionic acid derivatives and novel intermediate compounds

Provided is a process for preparing terbinafine or its HCl salt comprising: reacting a furan derivative with a base to form a second compound; performing a reductive alkylation of the second compound obtained in the step with N-methyl- -naphthalenemethylamine or its HCl salt to form a third compound; and purifying the third compound.

Process for preparing terbinafine and HCI salt thereof

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Gyeonggi-do, South Korea

Kyoung-Chan Kwon