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

Asymmetric synthesis of γ-chloro-α,β-diamino- and β,γ-aziridino-α-aminoacylpyrrolidines and -piperidines via stereoselective Mannich-type additions of N-(diphenylmethylene)glycinamides across α-chloro-N-sulfinylimines

• Gert Callebaut,
• Sven Mangelinckx,
• Pieter Van der Veken,
• Karl W. Törnroos,
• Koen Augustyns and
• Norbert De Kimpe

Beilstein J. Org. Chem. 2012, 8, 2124–2131, doi:10.3762/bjoc.8.239

• application of GLP-1 is problematic due to the lack of oral activity and the rapid degradation by plasma DPP IV. Therefore, DPP IV inhibitors could offer a solution to this problem, as they can extend the duration of action of GLP-1 and prolong the beneficial effects [10][11][12]. Besides DPP IV, a few

• related enzymes are present in the family of DPPs, with DPP II, DPP8, DPP9 and FAP being the most important regarding the therapeutic potential, when focusing on the inhibitory potency and selectivity [10][11][12]. In the research focused on DPP II and DPP IV inhibitors, it has been found that the α,γ

Synthesis of (S)-1-(2-chloroacetyl)pyrrolidine- 2-carbonitrile: A key intermediate for dipeptidyl peptidase IV inhibitors

• Santosh K. Singh,
• Narendra Manne and
• Manojit Pal

Beilstein J. Org. Chem. 2008, 4, No. 20, doi:10.3762/bjoc.4.20

• inhibitor Vildagliptin. Keywords: amides; DPP-IV inhibitors; L-proline; N-acylation; 2(S)-cyanopyrrolidine; Background One of the emerging and mechanism based approaches for the treatment of type-II diabetes is dipeptidyl peptidase IV (DPP-IV; CD26; E.C. 3.4.14.5) inhibition with the help of small

• molecules [1][2][3]. DPP-IV, a member of the prolyl oligopeptidase family of serine protease, cleaves the N-terminal dipeptide from peptides with proline or alanine in the second position. As a result of intense pharmaceutical research, several DPP-IV inhibitors have been discovered and a few of them

• GLP-1, which in turn enhances insulin secretion and improves the glucose tolerance. DPP-IV inhibitors offer several potential advantages over existing therapies including decreased risk of hypoglycemia, potential for weight loss, and the potential for regeneration and differentiation of pancreatic β