Inventing and understanding catalytic, enantioselective reactions

Masakatsu Shibasaki, Naoya Kumagai, Tomoyuki Mashiko

Research output: Contribution to journalReview articlepeer-review

8 Citations (Scopus)


This review summarizes recent advances in the development of efficient routes based on enantioselective catalysis for the synthesis of optically active therapeutic agents. Particular emphasis is placed on research that has streamlined the large-scale production of therapeutics for the treatment of type 2 diabetes mellitus (T2DM). Progress in the catalytic asymmetric hydrogenation and amination of unprotected substrates has enabled the establishment of concise synthetic routes for the production of the potent dipeptidyl peptidase 4 inhibitor sitagliptin, and the aldose reductase inhibitor ranirestat (Dainippon Sumimoto Pharma Co Ltd/Eisai Co Ltd/ Kyorin Pharmaceutical Co Ltd), both of which have attracted particular attention for their potential to treat T2DM and diabetic complications, respectively.

Original languageEnglish
Pages (from-to)862-875
Number of pages14
JournalCurrent Opinion in Drug Discovery and Development
Issue number6
Publication statusPublished - 2009 Nov
Externally publishedYes


  • Aldose reductase inhibitor
  • Amination
  • Asymmetric catalysis
  • Diabetes mellitus
  • Diabetic complications
  • Dipeptidyl peptidase 4 inhibitor
  • DPP-4 inhibitor
  • Hydrogenation
  • Lanthanum
  • Ranirestat
  • Sitagliptin

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery


Dive into the research topics of 'Inventing and understanding catalytic, enantioselective reactions'. Together they form a unique fingerprint.

Cite this