174652-94-9

Upstream product

• 614-16-4 Benzoylacetonitrile 
• 1188-33-6 N,N-dimethylformamide diethyl diacetal 
• 4637-24-5 N,N-dimethyl-formamide dimethyl acetal 
• 93-58-3 benzoic acid methyl ester 
• 1131-80-2 (E)-3-(N,N-dimethylamino)-1-phenyl-2-propen-1-one 
• 950851-57-7 ethyl 3-{[(N,N-dimethylamino)methylene]amino}-4-(4-methoxyphenyl)-6-methyl-1H-pyrazolo[3,4-b]pyridine-5-carboxylate 
• 1006-67-3 5-phenylisoxazole 

Downstream Products

• 174652-95-0 3-Benzylamino-2-cyano-1-phenyl-2-propen-1-one 
• 54606-37-0 (5-amino-1-phenyl-1H-pyrazol-4-yl)-phenyl-methanone 
• 7791-48-2 1,5-diphenyl-1H-pyrazole-4-carbonitrile 
• 264927-84-6 2-amino-5-cyano-4-phenylpyrimidine 
• 264927-73-3 7-phenyl-1,2,4-triazolo[1,5-a]pyrimidine-3-carbonitrile 
• 314268-89-8 5-Cyano-N-[4-(2-dimethylaminoethoxy)phenyl]-4-phenyl pyrimidine-2-amine 

Relevant academic research and scientific papers

Expedient synthesis of highly substituted 3,4-dihydro-1,2-oxathiine 2,2-dioxides and 1,2-oxathiine 2,2-dioxides: revisiting sulfene additions to enaminoketones

Diversely substituted 1,2-oxathiine 2,2-dioxides, including 3,5,6-triaryl-, 3,6-diaryl-, 3,5-diaryl-, 5,6-diaryl- and selected fused heterocyclic analogues, have been efficiently obtained by the application of a mild Cope elimination of a 4-amino moiety from the requisite 4-amino-3,4-dihydro-1,2-oxathiine 2,2-dioxides, which themselves were readily obtained by the addition of sulfenes to enaminoketones.

SUBSTITUTED DIAMINOPYRIMIDYL COMPOUNDS, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH

Provided herein are diaminopyrimidyl Compounds having the following structures: wherein X, L, R1, and R2 are as defined herein, compositions comprising an effective amount of a Diaminopyrimidyl Compound, and methods for treating or preventing PKC-theta-mediated disorders, or a condition treatable or preventable by inhibition of a kinase, for example, PKC-theta.

Facile iterative synthesis of 2,5-terpyrimidinylenes as nonpeptidic α-helical mimics

A facile iterative synthesis of 2,5-terpyrimidinylenes that are structurally analogous to α-helix mimics is presented. Condensation of amidines with readily prepared α,β-unsaturated α-cyanoketones gives 5-cyano-substituted pyrimidines. Iterative transformation of the 5-cyano group into an amidine allows synthesis of 2,5-terpyrimidinylenes with variable groups at the 4-, 4′-, and 4′′-positions. These compounds are designed to mimic the i, i + 4, and i + 7 sites of an α-helix.

ALPHA-HELIX MIMETIC USING A 2,5-OLIGOPYRIMIDINE SCAFFOLD

Alpha-helix mimetics and associated methods of making are provided. These compounds are constructed using a 2,5-oligopyrimidine scaffold. The semi-rigid scaffold holds individual side chain-like residues in orientations that mimic the orientations of side chain residues of an ?-helical protein domain. The new scaffold is easier to make than previous scaffolds and has much more favorable physical properties than previous alpha-helix mimics. The amphiphilic alpha-helix mimetics have application for making libraries and for treating diseases or conditions effected by the inhibition or disruption of interactions with the alpha helix of a protein.

Pyrazolo[3,4-b]pyridine in heterocyclic synthesis: Synthesis of new pyrazolo[3,4-b]pyridines, imidazo[1′,2′:1,5]pyrazolo[3,4-b] pyridines, and pyrido[2′,3′:3,4]pyrazolo[1,5-a]pyrimidines

Pyrazolo[3,4-b]pyridine derivatives 7 and 9 were synthesized via the reaction of 3-amino-1H-pyrazolo-[3,4-b]pyridine derivative 2 with ω-bromoacetophenones. Reaction of 7 and 9 with Ac2O afforded the imidazo[1′,2′:1,5]pyrazolo[3,4-b]pyridine derivative 8 and pyrazolo[3,4-b]pyridine derivative 10, respectively. Reaction of 2 with chloroacetonitrile followed by DMF-DMA gave imidazo[1′,2′:1,5] pyrazolo[3,4-b]pyridines 4 and 5, respectively. Acetylacetone and 1,1-dicyano-2,2-dimethylthioethene were reacted with 2 to afford the pyrido[2′,3′:3,4]pyrazolo-[1,5-a]-pyrimidines 11 and 14, respectively. Also, 2 reacted with DMF-DMA to yield the formamidine 15, which in turn, reacted with active methylene reagents, yielding the corresponding pyrido[2′,3′:3,4]pyrazolo[1,5-a]pyrimidines 18 and 23a-23d.

Pyrazolo[1,5-a]pyrimidin-7-yl phenyl amides as novel antiproliferative agents: Exploration of core and headpiece structure-activity relationships

A novel series of antiproliferative agents containing pyrazolo[1,5-a]pyrimidin-7-yl phenyl amides, selective for p21-deficient cells, were identified by high-throughput screening. Exploration of the SAR relationships in the headpiece, core, and tailpiece

Adenosine receptor ligands and their use in the treatment of disease

The invention relates to cyclic heteroaromatic compounds, containing at least one nitrogen atom, and to their use in the manufacture of medicaments for the treatment of diseases, related to adenosine receptor modulators, such as Alzheimer's disease, Parkinson's disease, neuroprotection, schizophrenia, anxiety, pain, respiration deficits, depression, asthma, allergic responses, hypoxia, ischaemia, seizure, substance abuse, sedation and they may be active as muscle relaxants, antipsychotics, anti epileptics, anticonvulsants and cardiaprotective agents.

New routes to the synthesis of pyridazinone, ethoxypyridine, pyrazole and pyrazolo[1,5-a]pyrimidine derivatives incorporating a benzotriazole moiety

A new approach to the synthesis of pyridazinone, ethoxypyridine, pyrazole and 7-aminopyrazolo-[1,5-a]pyrimidine derivatives. The structure of the newly synthesized compounds was elucidated by elemental analyses, ir, 1H nmr spectra and in some cases by 13C nmr investigations.

Synthesis of New Azoloazine Derivatives: New Routes to 1,2,4-Triazolo[4,3-a]pyrimidines, Pyrazolo[1,5-a]pyridines and Pyrazolo[3,4-b]pyridinones

Azoloazines are produced via reacting aminoazoles with enaminones, enaminonitriles and with ethyl alkylidene cyanoacetate.

Steric and electronic control in the addition of hydrazine and phenylhydrazine to α-[(dimethylamino)methylene]-β-oxoarylpropanenitriles

Reaction of hydrazine with α-[(dimethylamino)methylene]-β-oxoarylpropanenitriles 2 gives a mixture of the 4-aroyl-5-aminopyrazoles 3 and the 5-aryl-4-cyanopyrazoles 4. Similarly reaction of 2 with phenylhydrazine gives rise to the 5-amino-4-aroyl-1-phenylpyrazoles 5 and 5-aryl-4-cyano-1-phenylpyrazoles 6. The regioselectivity of addition has been investigated with respect to the electronic nature and steric requirements of the aromatic substitution. The ratio of products was found to be independent of the electronic nature of the substituent. The outcome of the reaction was however very sensitive to steric factors. Substituents in the para- and meta-positions favoured formation of the pyrazole-nitrile products 4 and 6, whereas sterically demanding ortho-substituents favoured the pyrazole-amino ketones 3 and 5.