1449657-47-9Relevant academic research and scientific papers
Purine compound, intermediate, preparation method and its application
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Paragraph 0074-0076, (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.
Synthesis and biological evaluation of xanthine derivatives on dipeptidyl peptidase 4
Lin, Kuaile,Cai, Zhengyan,Wang, Fei,Zhang, Wei,Zhou, Weicheng
, p. 477 - 482 (2013/05/22)
A series of xanthine derivatives in which a methylene was inserted at position 8 of xanthine scaffold was synthesized and evaluated as inhibitors of dipeptidyl peptidase 4 (DPP-4) for the treatment of type 2 diabetes. As the results of structure-activity relationship (SAR) study of the series, the compounds with 4-methylquinazoline- 2-yl-methyl group at N-1 position and 2-aminoethylaminomethyl group gave better activities. Compounds H4 and H9 showed good DPP-4 inhibition and more than 100-fold selectivity over DPP-7 and DPP-8.
