7759-03-7

Upstream product

• 80-18-2 Methyl benzenesulfonate 
• 94-02-0 ethyl 3-oxo-3-phenylpropionate 
• 18107-18-1 diazomethyl-trimethyl-silane 
• 623-73-4 diazoacetic acid ethyl ester 
• 93-58-3 benzoic acid methyl ester 
• 927-80-0 1-ethoxyacetylene 

Downstream Products

• 116429-07-3 3-methoxy-3-phenylpropenic acid 
• 1374217-69-2 6-phenyl-1,5-dihydropyrido[3,2-d]pyrimidine-2,4,8-trione 
• 1374217-91-0 2-benzylsulfanyl-4,6-diphenyl-8-chloropyrido[3,2-d]pyrimidine 
• 1374217-94-3 2-chloro-4,6-diphenyl-8-benzylsulfanylpyrido[3,2-d]pyrimidine 
• 1374217-75-0 2,8-dichloro-4,6-diphenylpyrido[3,2-d]pyrimidine 
• 1374217-73-8 2,8-dichloro-4-methylsulfanyl-6-phenylpyrido[3,2-d]pyrimidine 

Relevant academic research and scientific papers

Structure-activity studies of a series of dipyrazolo[3,4-b:3′,4′-d]pyridin-3-ones binding to the immune regulatory protein B7.1

The interaction of co-stimulatory molecules on T cells with B7 molecules on antigen presenting cells plays an important role in the activation of naive T cells. Consequently, agents that disrupt these interactions should have applications in treatment of transplant rejection as well as autoimmune diseases. To this end, specific small molecule inhibitors of human B7.1 were identified and characterized. Herein, we report the identification of potent small molecule inhibitors of the B7.1-CD28 interaction. In a high-throughput screen we identified several leads that prevented the interaction of B7.1 with CD28 with activities in the nanomolar to low micromolar range. One of these, the dihydrodipyrazolopyridinone 1, was subsequently shown to bind the V-like domain of human B7.1 at equimolar stoichiometry. With this as a starting point, we report here the synthesis and initial in vitro structure-activity relationships of a series of these compounds.

Chromium-copper exchange of Fischer carbene complexes: X-ray crystal structure of a [Cu{=CR1(OR2)}(MeCN)(Et2O)][PF6] complex

The chromium-copper interaction is evidenced for chromium-carbene complexes and Cu+ in the CuBr-catalyzed cross-coupling reaction of ethyl diazoacetate (EDA) and Fischer alkoxycarbene - chromium complexes (see scheme). In contrast, with [Cu(MeCN)4][PF6] (0.5 equiv) instead of CuBr a carbene ligand exchange between a chiral alkenylchromium carbene complex (R1 = (E) CH=CH-2-furyl, R2 = (1R, 2S, 5R)-menthyl) and this Cu compound occurs at room temperature. The resulting novel trigonal-planar copper(I) - carbene complex, which contains MeCN and Et2O as the remaining ligands, has been isolated and structurally characterized by X-ray diffraction.

MESOMERIC ANIONS. X. METHYLATION OF ALKALI-METAL DERIVATIVES OF SOME 1,3-KETONITRILES

The effect of polar factors on the relative nucleophilicity of the oxygen and carbon reaction centers in the alkali-metal derivatives of 2-(X-benzoyl)acetonitriles, 2-(X-benzoyl)propionitriles, and 2-(X-phenyl)acetylacetonitriles was investigated.During methylation with methyl iodide and methyl p-toluenesulfonate in DMFA the ratio of the C- and O-methylation products for all the investigated compounds decreases with increase in the accepting power of the substituent X.It was shown that the sensitivity of the C-reaction center to the effect of the substituent X is greater than that of the O-center.