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  • 【Research Achievements】A paper was published in Organic Process Research & Development

【Research Achievements】A paper was published in Organic Process Research & Development


A paper by Masatoshi Yamada and others of the Pharmaceutical Research Division has been published in the academic journal “Organic Process Research & Development” of the American Chemical Society.

【Details of the paper】
Journal: Organic Process Research&Development
Title: Development and Scale-Up of an Asymmetric Synthesis Process for Alogliptin
Publication date: February 10, 2021
Authors: Masatoshi Yamada*, Sayuri Hirano, Ryoji Tsuruoka, Masahiro Takasuga, Kenichi Uno, Kotaro Yamaguchi and Mitsuhisa Yamano


Summary: A paper has been published on the asymmetric synthesis of alogliptin, a type 2 diabetes drug that was developed during the Takeda era. An efficient and eco-friendly synthesis was achieved by synthesizing an optically active amine from an inexpensive nicotinic acid derivative as raw material using an asymmetric hydrogenation reaction, followed by a condensation reaction with the corresponding parent core structure and finally obtaining alogliptin through use of a sophisticated Hofmann rearrangement.

The research started during the Takeda Pharmaceutical Company era, but the key asymmetric synthesis technology has been transferred to SPERA PHARMA. We will continue to utilize the technology and the vast experience, to support customers in solving their problems and contribute to the swift creation of pharmaceutical products.

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