The present invention relates to a preparation method of sitagliptin, and more particularly, to a method of preparing sitagliptin using L-aspartic acid having a (R)-beta amino acid structure by mild amide formation, by the use of industrially applicable halo isopropylmagnesium, and by removal of amine protecting group using Pd/C and H2 and carbonyl reduction using reducing agent.
申请公布号
WO2012148246(A2)
申请公布日期
2012.11.01
申请号
WO2012KR03381
申请日期
2012.04.30
申请人
DAEWOONG PHARMACEUTICAL CO., LTD.;CHOI, SOO JIN;LEE, BYUNG GOO;OH, SEONG SOO;KIM, YONG TAE;EO, JIN YONG;KIM, HUNG SOP
发明人
CHOI, SOO JIN;LEE, BYUNG GOO;OH, SEONG SOO;KIM, YONG TAE;EO, JIN YONG;KIM, HUNG SOP