52208-82-9Relevant articles and documents
Purine compound, intermediate, preparation method and its application
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Paragraph 0093; 0095-0096, (2017/01/23)
The invention discloses a xanthine compound I, wherein R1 is 2-cyanophenyl or hydrogen; R2 is 2-cyanobenzyl; R3 is amino or wherein n=2-4, m=2-3, D is H or NH2 and E is CH2 or NH. A preparation method of the xanthine compound I comprises the following steps of: performing nucleophilic substitution reaction on a compound II and R3H; or (1) performing the nucleophilic substitution reaction on the compound II and R-3-tert-oxyacyl aminopiperidine; and (2) removing a tert-oxyacyl protecting group. The invention further discloses any intermediate of the xanthine compound I, wherein R1 and R2 are as described above. The invention further relates to an application of the xanthine compound I in preparation of a DPP-4 (dipeptidyl peptidase-4) enzyme activity inhibitor or medicaments for treating and/or preventing relevant diseases by inhibiting a DPP-4 enzyme. The xanthine compound I disclosed by the invention provides a new direction for research and development of the DPP-4 inhibitor, and has important significance in development of the potential DPP-4 inhibitors. Formula III, formula II and formula I are shown in the specification.