848665-64-5

Upstream product

• 79-03-8 propionyl chloride 
• 555-21-5 4-Nitrophenylacetonitrile 
• 33279-01-5 3-oxo-pentanenitrile 
• 586-78-7 para-nitrophenyl bromide 

Downstream Products

• 885428-60-4 (Z)-3-Methoxy-2-(4-nitro-phenyl)-pent-2-enenitrile 
• 848666-40-0 3-[2,6-diamino-5-(4-nitro-phenyl)-pyrimidin-4-yl]-propionic acid methyl ester 
• 71552-34-6 6-ethyl-5-(4'-nitrophenyl)-pyrimidine-2,4-diamine 
• 502136-76-7 5-(4'-aminophenyl)-6-ethyl-pyrimidine-2,4-diamine 
• 861103-13-1 6-Ethyl-5-[4-(4-methanesulfonyl-benzylamino)-phenyl]-pyrimidine-2,4-diamine 
• 885425-61-6 1-(4-{[4-(2,4-diamino-6-ethyl-pyrimidin-5-yl)-phenylamino]-methyl}-phenyl)-ethanone 

Relevant academic research and scientific papers

Preparation of 3,4-Substituted-5-Aminopyrazoles and 4-Substituted-2-Aminothiazoles

3,4-Substituted-5-aminopyrazoles and 4-substituted-2-aminothiazoles are frequently used intermediates in medicinal chemistry and drug discovery projects. We report an expedient flexible synthesis of 3,4-substituted-5-aminopyrazoles (35 examples), based on palladium-mediated α-arylation of β-ketonitriles with aryl bromides. A library of 4-substituted-2-aminothiazoles (21 examples) was assembled by a sequence employing Suzuki coupling of newly prepared, properly protected pinacol ester and MIDA ester of 4-boronic acid-2-aminothiazole with (hetero)aryl halides.

2,4-Diaminopyrimidine derivatives as potent growth hormone secretagogue receptor antagonists

Ghrelin, a gut-derived orexigenic hormone, is an endogenous ligand of the growth hormone secretagogue receptor (GHS-R). Centrally administered ghrelin has been shown to cause hunger and increase food intake in rodents. Inhibition of ghrelin actions with ghrelin antibody, peptidyl GHS-R antagonists, and antisense oligonucleosides resulted in weight loss and food intake decrease in rodents. Here we report the effects of GHS-R antagonists, some of which were potent, selective, and orally bioavailable. A structure-activity relationship study led to the discovery of 8a, which was effective in decreasing food intake and body weight in several acute rat studies.

Pyrimidine derivatives as ghrelin receptor modulators

The present invention is related to compounds of formula (I), or a therapeutically suitable salt or prodrug thereof, the preparation of the compounds, compositions containing the compounds and the use of the compounds in the prevention or treatment of disorders regulated by ghrelin including anorexia, cancer cachexia, eating disorders, age-related decline in body composition, weight gain, obesity, and diabetes mellitus.

Diaminopyrimidine derivatives as growth hormone secrectgogue receptor (GHS-R) antagonists

The present invention is related to compounds of formula (I), or a therapeutically suitable salt or prodrug thereof, the preparation of the compounds, compositions containing the compounds and the use of the compounds in the prevention or treatment of disorders regulated by the action of ghrelin receptor, including Prader-Willi syndrome, eating disorder, weight gain, weight-loss maintainance following diet and exercise, obesity, and disorders associated with obesity such as noninsulin dependent diabetes mellitus.