Related substance of linagliptin intermediate and synthesis method thereof
US12122754B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Jun 9, 2021 |
| Grant date | Oct 22, 2024 |
| Priority date | — |
| Expiry date | Apr 17, 2043 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D239/74
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
A related substance of linagliptin intermediate 2-(chloromethyl)-4-methylquinazoline, 4,4′-(2-methylpropane-1,3-diyl)bis(2-(chloromethyl)quinazoline) and a method for synthesizing the related substance (impurity) by reacting 2-(chloromethyl)-4-methylquinazoline with acetaldehyde under an alkaline condition and a purification method are provided. The preparation method is simple and convenient to operate, short in reaction time, high in product purity, and high in yield. The synthesized related substance can be used for qualitative and quantitative analysis of the linagliptin intermediate 2-(chloromethyl)-4-methylquinazoline and API impurities of linagliptin, so that the medication safety of the linagliptin is improved.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.