Work

Practical asymmetric hydrogenation of tetrasubstituted cyclic enamides for enantioenriched 3-amino-4-methylpiperidines

Year: 2026

Type: article

Abstract: balloon at room temperature. A broad range of substrates was well tolerated, affording the corresponding products in up to 96% yield and 99% ee. The catalytic system showed high efficiency, achieving a turnover number of 10 000 on gram scale. The utility of the method was further demonstrated by the preparation of a key intermediate for the formal synthesis of tofacitinib. This practical and scalable protocol provides efficient access to chiral 3-amino-4-methylpiperidines and expands the scope of asymmetric hydrogenation of highly substituted enamides.

Source: Chemical Science

DOI: 10.1039/d6sc05491a

Authors: Qishu Chen, Qin Feng, Xiuxiu Li, Congcong Yin, Xumu Zhang

Institution: Southern University of Science and Technology

Language: English

Topic: Asymmetric Hydrogenation and Catalysis

Subfield: Inorganic Chemistry

Field: Chemistry

Domain: Physical Sciences

Open Access status: diamond

Funders: Southern University of Science and Technology, National Key Research and Development Program of China

Award: G2965680878