475995-40-5

Upstream product

• 1670-14-0 benzamidine monohydrochloride 
• 874-42-0 2,4-dichlorobenzaldeyhde 
• 109-77-3 malononitrile 
• 2972-76-1 2-(2,4-dichlorobenzylidene)malononitrile 
• 618-39-3 benzamidin 

Relevant academic research and scientific papers

A novel and efficient synthesis of pyrazolo[3,4-d]pyrimidine derivatives and the study of their anti-bacterial activity

In this work 4-amino-6-aryl-2-phenyl pyrimidine-5-carbonitrile derivatives were synthesized through a one-pot, three-component reaction of an aldehyde, malononitrile and benzamidine hydrochloride, in the presence of magnetic nano Fe3O4 particles as a catalyst under solvent-free conditions. 3-Amino-6-aryl-2-phenylpyrazolo[3,4-d]pyrimidine derivatives were prepared through an efficient and environmentally friendly reaction between 4-amino-6-aryl-2-phenylpyrimidine-5-carbonitrile derivatives and hydrazine hydrate and their antibacterial activity has been evaluated.

A facile synthesis of new pyrazolo[3,4-d]pyrimidine derivatives via a one-pot four-component reaction with sodium acetate supported on basic alumina as promoter

An efficient one-pot procedure for the synthesis of 3-amino-6-aryl-2- phenylpyrazolo[3,4-d]pyrimidine derivatives, through the reaction of aldehydes, malononitrile, benzamidine hydrochloride, and hydrazine hydrate in the presence of basic alumina-supported sodium acetate (AcONa/Al2O3) under reflux conditions, is reported. This protocol has some advantages, including the use of a simple and one-pot synthetic approach to attain pyrazolo[3,4-d]pyrimidine directly from four readily available starting materials, simple workup, high overall yields of the products, and the simultaneous conversion of a NO2 to an amino group, offering an opportunity to synthesize more complex structures. Copyright

Aminomethylpyrimidines as novel DPP-IV inhibitors: A 105-fold activity increase by optimization of aromatic substituents

The influence of aromatic substitution on a newly discovered class of inhibitors of dipeptidyl peptidase IV was investigated. A 105-fold increase in potency was achieved by the optimization of aromatic substituents in a parallel chemistry progr

An aminomethylpyrimidine DPP-IV inhibitor with improved properties

A recently identified DPP-IV inhibitor (1) was found to induce phospholipidosis and to inhibit CYP3A4. A small series of less lipophilic and less amphiphilic analogues was synthesized in an effort to overcome these issues. One compound from this series was equipotent to 1, did not induce phospholipidosis and showed a reduced CYP3A4 inhibition.

Pyridine and pyrimidine derivatives

The present invention provides compounds of formula (I) wherein R1, R2, R3, R4 and X are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment

Synthesis of new 4-amino-2,6-diarylpyrimidine-5-carbonitriles

A facile synthesis of the title compounds 5a-e, from appropriate amidines and benzylidenemalononitriles, is described.