Abstract:
The present invention relates to a novel and improved process for the preparation of linagliptin, chemically known as (R)-8-(3-amino-piperidin-l-yl)-7-but-2-ynyl-3-methyl-l-(4-methyl-quinazolin-2-ylmethyl)-3, 7-dihydro-purine-2, 6-dione through novel intermediates using (3S)-l-(7-(but-2-ynyl)-3-methyl-l-((4-methylquinazolin-2-yl)methyl)-2, 6-dioxo-2, 3, 6, 7-tetrahydro-lH-purin-8-yl) piperidin-3-yl methanesulfonate (K) and (3R)-8-(3-azidopiperidin-l-yl)-7-(but-2-ynyl)-3-methyl-l-((4-methylquinazolin-2-yl)methyl)-1 H-purine-2,6-(3H,7H)-dione (L).