Yuhan Corporation

Doo-Byung Lee

Hyun Ju

Ja-Heouk Khoo

Woo-Seob Shin

Jun-Sup Lee

Sang-Ho Oh

Jong-Chul Lim

Jung-Ae Lee

Sang-Seol Jeon

Ji-Hye Choi

Tai-Au Lee

Kyoung-Chan Kwon

Jeong-Seok Chae

Beom-Joo Maeng

Kyeong-Sill Lee

Hyo-Ick Hwang

Ik-Su Jo

Su-Young Lee

Sang-Won Kim

Sung-Hee Cho

Sang-Seon Park

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 provides a novel process for preparing a diaminopyrimidine derivative or acid addition salt thereof having an activity as a 5-HTreceptor agonist. And also, the present invention provides novel crystalline forms of a hydrochloride of the diaminopyrimidine derivative and processes for preparing the same.

Processes for preparing a diaminopyrimidine derivative or acid addition salt thereof

Provided are a novel process for preparing a diaminopyrimidine derivative or acid addition salt thereof having an activity as a 5-HTreceptor agonist, crystalline forms of a hydrochloride of the diaminopyrimidine derivative, and processes for preparing the same.

The present invention provides intermediates useful for the synthesis of an aminopyrimidine derivative or pharmaceutically acceptable salt thereof having a selective inhibitory activity against protein kinases, especially against the protein kinases for mutant epidermal growth factor receptors; and processes for preparing the same. And also, the present invention provides novel intermediates useful for said process and processes for preparing the same.

Intermediates useful for the synthesis of a selective inhibitor against protein kinase and processes for preparing the same

The present invention provides a novel process for preparing an aminopyrimidine derivative or pharmaceutically acceptable salt thereof having a selective inhibitory activity against protein kinases, especially against the protein kinases for mutant epidermal growth factor receptors. And also, the present invention provides novel intermediates useful for said process and processes for preparing the same.

Intermediates useful for the synthesis of aminopyrimidine derivatives, process for preparing the same, and process for preparing aminopyrimidine derivatives using the same

The present invention provides a process for preparing an imidazole derivative or its salt which comprises reacting a tetrahydrofuran or tetrahydropyran derivative with formamidine or its salt in the presence of a base.

Processes for preparing imidazole derivatives and salts thereof

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Gyeonggi-do, South Korea

Doo-Byung Lee