13182-96-2

Upstream product

• 3034-38-6 1H-4⁽⁵⁾-nitroimidazole 
• 107-13-1 acrylonitrile 
• 2417-90-5 bromopropionitrile 

Downstream Products

• 3034-42-2 1-methyl-5-nitro-1H-imidazole 
• 215099-39-1 1-(2-Cyanoethyl)-4-aminoimidazole 

Relevant academic research and scientific papers

Polystyrene-supported CuI-imidazole complex catalyst for aza-Michael reaction of imidazoles with α,β-unsaturated compounds

The polystyrene-supported CuI-imidazole complex catalyst was prepared and characterized by IR spectroscopy, elemental analysis, SEM/TEM and TG/DSC. The complex catalyst was globular with the size of 400-500 nm and showed a good thermal stability at high temperature. The immobilized Cu metal in the complex catalyst was about 0.85 mmol/g. By using the catalyst, aza-Michael reaction of imidazoles to α,β-unsaturated compounds was performed with good yields in 4-8 h. The catalyst showed an excellent recycling efficiency over five cycles without distinct leaching of metal from the polymer support.

Synthesis and biological results of the technetium-99m-labeled 4-nitroimidazole for imaging tumor hypoxia

1-(4-Nitroimidazole-1-yl)-propanhydroxyiminoamide (N4IPA) was synthesized. The biodistribution of 99mTc-N4IPA in mice bearing S180 tumor demonstrated that the complex showed accumulation in tumor and slow clearance from it. The tumor-to-tissue uptake ratios increase with time. These results suggest that 99mTc-N4IPA would be a marker for imaging tumor hypoxia.

Preparation and biological evaluation of 99mTc-N4IPA for single photon emission computerized tomography imaging of hypoxia in mouse tumor

In order to develop technetium-99m labeled nitroimidazole imaging agent for hypoxia in tumor, we have synthesized 99mTc-1-(4-nitroimidazole-yl)- propanhydroxyiminoamide, 99mTc-N4IPA complex, in high radiochemical purity and radiochem

Method for catalytically synthesizing N, N'-disubstituted urea derivative and imidazole derivative

The present invention relates to a green and efficient method for preparing an N, N'-disubstituted urea derivative and an imidazole derivative. The method for preparing the N, N'-disubstituted urea derivative by condensation of an aromatic amine with a carbonate ester comprises: by using ionic liquid loaded magnetic nanoparticles as a catalyst, at the temperature of 60-100 DEG C, and at a normal pressure, and in a condition of solvent-free, performing a condensing reaction on the aromatic amine and the carbonate ester for 8-14 hours to obtaina corresponding N, N'-disubstituted urea derivative; by using a magnetic nanoparticle-loaded ionic liquid as a catalyst and by using ethanol as a solvent, performing Michael addition reaction of a substituted imidazole and an electron-deficient olefin for 1-5 hours at the temperature of 10-50 DEG C and at a normal pressure to obtain a corresponding imidazole derivative, wherein the catalyst is as shown in the specification. Experiments verify that after the reaction is completed, the catalyst is recycled simply through an external magnetic field and can be repeatedly used for many times, but the activity is not obviously reduced. The catalytic system is simple in operation and high in yield, and the reusability is good, so that the method has a good industrial prospect.

Triethylammonium acetate (TEAA): A recyclable inexpensive ionic liquid promotes the chemoselective aza- and thia-Michael reactions

A new, highly efficient, inexpensive, recyclable, mild, convenient, and green protocol for chemoselective aza/thia-Michael addition reactions of amines/thiols to α,β-unsaturated compounds using triethylammonium acetate (TEAA) ionic liquid was developed. The catalyst can be recycled ten times and obviate the need for toxic and expensive catalysts.

A fast and highly efficient protocol for Michael addition of N-heterocycles to α,β-unsaturated compound using basic ionic liquid [bmIm]OH as catalyst and green solvent

A fast and green protocol for the Michael addition of N-heterocycles to α,β-unsaturated compounds at room temperature was developed using a basic ionic liquid, 1-methyl-3-butylimidazolium hydroxide, [bmIm]OH, as a catalyst and a reaction medium. The react

Promiscuous acylase-catalyzed aza-Michael additions of aromatic N-heterocycles in organic solvent

A novel and efficient enzymatic promiscuous protocol for aza-Michael addition of aromatic N-heterocycles to α,β-unsaturated compounds has been described. The reactions were catalyzed by promiscuous zinc-active-site acylase in organic solvent at 50 °C. The strategy works with a broad range of N-heterocycles to afford the corresponding Michael adduct with good yields in several hours (0.5-6 h). This catalytic promiscuity is the first example of metal-active-site enzyme-catalyzed aza-Michael addition for aromatic N-heterocycles.

Epoxysuccinamide derivative or salt thereof

PCT No. PCT/JP98/01778 Sec. 371 Date Dec. 17, 1998 Sec. 102(e) Date Dec. 17, 1998 PCT Filed Apr. 17, 1998 PCT Pub. No. WO98/47887 PCT Pub. Date Oct. 29, 1998The invention relates an epoxysuccinamide derivative represented by a formula (I): wherein R1 represents a hydrogen atom, an alkyl or aminoalkyl group, R2 represents an aminoalkyl group which May be substituted, an aryl group which may be substituted, a heterocyclic group which may be substituted, an aralkyl group which may be substituted, or an alkyl group substituted by a heterocyclic ring which may be substituted, or R1 and R2 may form a nitrogen-containing heterocyclic ring, which may be substituted, together with the adjacent nitrogen atoms, and R3 and R4 are the same or different from each other and independently represent a hydrogen atom, or an alkyl or aralkyl group, or a salt thereof, a preparation process thereof, and a medicine comprising such a derivative or salt as an active ingredient. This compound has a specific inhibitory activity for cathepsin L and family enzymes thereof, and is useful as an agent for preventing and treating metabolic osteopathy such as osteoporosis and hypercalcemia.

Catalysis and regioselectivity in the Michael addition of azoles. Kinetic vs. thermodynamic control

Bicyclic guanidine bases, TBD and MTBD were found to be high]y efficient catalysts in the Michael addition of azoles with α,β-unsaturated nitriles and esters. The factors influencing regioselectivity have been elucidated, and some new azole-Michael adduct