1246610-77-4

Upstream product

• 21236-97-5 3-methyl-6-aminouracil 
• 1246610-78-5 3-(2-cyanoacetyl)-3-methyl-1-(2-cyanobenzyl)urea 

Downstream Products

• 1246610-74-1 2-[[6-[(3R)-3-tert-butoxycarbonylamino-1-piperidinyl]-3,4-dihydro-2,4-dioxo-3-methyl-1(2H)-pyrimidinyl]methyl]benzonitrile 

Relevant academic research and scientific papers

DPP-4 inhibitor with dual action mechanisms and application of DPP-4 inhibitor

The invention discloses a DPP-4 inhibitor with dual action mechanisms and application of the DPP-4 inhibitor, relates to the field of dipeptidyl peptidase IV inhibitor medicines and in particular relates to a DPP-4 inhibitor, a preparation method of a compound of formula I and medicinal application of the compound as a novel DPP-4 inhibitor, and particularly application of the inhibitor in preparing anti-diabetic medicines. In-vivo and in-vitro pharmacodynamic experiment results show that the compound of formula I has a remarkable inhibition function on DPP-4, has an excellent blood sugar reduction effect, and in addition has a relatively good action effect when being compared with similar medicines alogliptin and vildagliptin. Meanwhile, the compound disclosed by the invention is simple and short in preparation route, easy in raw material obtaining, simple in process, applicable to industrial large-scale production and very great in development prospect.

PROCESS FOR THE PREPARATION OF ALOGLIPTIN

The present invention is based on the discovery of a process for preparing pyrimidin- dione compounds, especially alogliptin and its derivatives, which comprises the reaction of a urea derivative of formula (VIII) with a malonic acid or its derivatives to form intermediates of formulae (VII) or (VII-A), which are subsequently converted to a compound of formula (II) upon introduction of a leaving group X. Compound (II) then reacts with an amine to form compound (I), which is optionally converted to its salts of formula (IV).