Yuhan Corporation

Sang-Ho Oh

Hyun Ju

Ja-Heouk Khoo

Woo-Seob Shin

Jong-Chul Lim

Su-Min Park

Dae-Gyu Park

Seong-Ran Lee

Yoon-Ah Hwang

Doo-Byung Lee

Jun-Sup Lee

Jung-Ae Lee

Sang-Seol Jeon

Ji-Hye Choi

Kyoung-Chan Kwon

Su-Young Lee

Kyeong-Sill Lee

Hyo-Ick Hwang

Ik-Su Jo

Sang-Won Kim

Sung-Hee Cho

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 an improved 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. Additionally, the present invention provides novel intermediates useful for said process and processes for preparing the same.

Process for preparing aminopyrimidine derivatives

The present invention provides an improved 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. Additional, the present invention provides novel intermediates useful for said process 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 an improved 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.

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

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Gyeonggi-do, South Korea

Sang-Ho Oh