Affiliation:
1. School of Perfume and Aroma Technology, Shanghai Institute of Technology, 120 Caobao Rd. Shanghai 200235, P. R. China
Abstract
An efficient asymmetric synthesis of Sitagliptin, a new DPP-IV inhibitor for the treatment of type 2 diabetes mellitus has been developed. The beta-amino acid fragment of Sitagliptin was prepared by asymmetric Michael addition of the corresponding α, β-unsaturated ester to (R)-(α-methylbenzyl)benzylamine followed by a two-step elaboration to obtain N-boc beta-amino ester. Hydrolysis of the ester and coupling with the triazolopiperazine afforded Sitagliptin after cleavage of the N-boc group and salt formation. The overall yield was 31% over nine steps.
Reference10 articles.
1. Robbins and Cotran pathologic basis of disease, 7th edn, 2004, Saunders, Philadelphia, pp 1194.
2. Dipeptidyl Peptidase IV Inhibitors for the Treatment of Diabetes
3. Therapeutic potential of dipeptidyl peptidase IV inhibitors for the treatment of type 2 diabetes
4. (2R)-4-Oxo-4-[3-(Trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin- 7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: A Potent, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes
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