1363383-00-9

Upstream product

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• 1206825-06-0 imidazo[2,1-f][1,2,4]triazin-4(3H)-one 
• 1206825-03-7 4-chloroimidazo[1,2-f][1,2,4]triazine 
• 3473-63-0 formamidine acetic acid 

Relevant academic research and scientific papers

Mechanism and structure based design of inhibitors of AMP and adenosine deaminase

Inhibitors of the enzyme adenosine monophosphate deaminase (AMPD) show interesting levels of herbicidal activity. An enzyme mechanism-based approach has been used to design new inhibitors of AMPD starting from nebularine (6) and resulting in the synthesis of 2-deoxy isonebularine (16). This compound is a potent inhibitor of the related enzyme adenosine deaminase (ADA; IC50 16 nM), binding over 5000 times more strongly than nebularine. It is proposed that the herbicidal activity of compound 16 is due to 5?-phosphorylation in planta to give an inhibitor of AMPD. Subsequently, an enzyme structure-based approach was used to design new non-ribosyl AMPD inhibitors. The initial lead structure was discovered by in silico screening of a virtual library against plant AMPD. In a second step, binding to AMPD was further optimised via more detailed molecular modeling leading to 2-(benzyloxy)-5-(imidazo[2,1-f][1,2,4]triazin-7-yl)benzoic acid (36) (IC50 300 nM). This compound does not inhibit ADA and shows excellent selectivity for plant over human AMPD.

HETEROCYCLIC DERIVATIVES AS PI3K INHIBITORS

This application relates to compounds of Formula (I): or pharmaceutically acceptable salts thereof, which are inhibitors of PI3K-γ which are useful for the treatment of disorders such as autoimmune diseases, cancer, cardiovascular diseases, and neurodegen

A process for preparing 7-bromo imidazo [2,1-f] [1, 2, 4] triazin-4-amine method

The invention discloses a method for preparing 7-bromoimidazo[2,1-f][1,2,4]triazin-4-amine. According to the invention, a compound IX is adopted as a a raw material, and is subjected to a reaction with a compound X under the effect of alkali, such that a