Process for the preparation of dipeptidylpeptidase inhibitors
US9353114B2 · kind B2 · utility
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8Claims
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Key dates
| Filing date | Aug 6, 2013 |
| Grant date | May 31, 2016 |
| Priority date | — |
| Expiry date | Aug 6, 2033 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D473/06
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Provided is a process for the preparation of linagliptin of Formula I, comprising deprotecting a compound of Formula II wherein R1 and R2 together with the nitrogen to which they are attached form a phthalimido group, wherein the aromatic ring of the phthalimido group is substituted with one or more R3 substituents selected from the group consisting of halogen, alkyi, nitro and amino; or R1 is H and R2 is selected from the group consisting of trialkylsilyl, 2-trialkylsilylethoxycarbamates, acetyl, trihaloacetyl, 9-fluorenylmethoxycarbonyl, trityl, alkylsulfonyl, arylsulfonyl, diphenylphosphine and sulfonylethoxycarbonyl.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.