On the application of 3d metals for C–H activation toward bioactive compounds: The key step for the synthesis of silver bullets

• Renato L. Carvalho,
• Amanda S. de Miranda,
• Mateus P. Nunes,
• Roberto S. Gomes,
• Guilherme A. M. Jardim and
• Eufrânio N. da Silva Júnior

Beilstein J. Org. Chem. 2021, 17, 1849–1938, doi:10.3762/bjoc.17.126

• in 57% yield (1:1 dr, Scheme 18C). Nitrogen-containing heterocycles are present in several valuable bioactive compounds, such as piracetam (50) [132], anisomycin (51) [133], and alogliptin (52) [134] (Scheme 20A). Sometimes better biological results are observed after simple structural modifications

Asymmetric synthesis of a high added value chiral amine using immobilized ω-transaminases

• Antonella Petri,
• Valeria Colonna and
• Oreste Piccolo

Beilstein J. Org. Chem. 2019, 15, 60–66, doi:10.3762/bjoc.15.6

• mainly used for the synthesis of dipeptidyl peptidase IV (DPP-IV) inhibitors, such as alogliptin, linagliptin and other antidiabetic agents [15][17]. Over the years, numerous synthetic pathways were tested for the preparation of 3-aminopiperidine and its N-protected precursors in an optically active form

Synthesis of a novel analogue of DPP-4 inhibitor Alogliptin: Introduction of a spirocyclic moiety on the piperidine ring

• Arumugam Kodimuthali,
• Padala Lakshmi Prasunamba and
• Manojit Pal

Beilstein J. Org. Chem. 2010, 6, No. 71, doi:10.3762/bjoc.6.71

• , Hyderabad 500 007, India Present address: Institute of Life Science, University of Hyderabad Campus, Gachibowli, Hyderabad 500 046, Andhra Pradesh, India 10.3762/bjoc.6.71 Abstract We report the synthesis of a novel analogue of Alogliptin via condensation of two key intermediates one of which is an

• aminopiperidine derivative bearing a spirocyclic ring on the piperidine moiety. Preparation of the aminopiperidine intermediate was carried out by constructing the cyclopropyl ring prior to assembling the piperidine ring. Keywords: Alogliptin; cyclopropyl ring; DPP-4; piperidine; Introduction Inhibition of

• . Several other inhibitors are in various stages of development. For example, Alogliptin or (2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]benzonitrile) (A, Figure 1), a potent (IC50 < 10 nM) and selective inhibitor (selectivity > 10,000 over DPP-8 and 9) is