102297-41-6Relevant articles and documents
Chemoselective: N-tert -butyloxycarbonylation of amines in glycerol
Ingale, Ajit P.,More, Vishal K.,Gangarde, Uddhav S.,Shinde, Sandeep V.
, p. 10142 - 10147 (2018)
A catalyst-free, efficient and green protocol has been developed for the chemoselective N-Boc protection of amines by using glycerol as a solvent at room temperature. A variety of functionalized amines, such as aliphatic, aromatic as well as heteroaromatic were protected using the developed protocol. N-tert-Butyloxycarbonylation derivatives were formed without the formation of isocyanate, urea, N,N-di-t-Boc, or oxazolidinone as side products. The operational simplicity, cleaner reaction, rapid reaction convergence, functional group tolerance, excellent yield, high selectivity, catalyst-free feature and solvent recyclability are the distinct advantages of this protocol. Owing to these merits, this protocol is feasible, economical and environmentally benign.
Sulfated tungstate: A highly efficient, recyclable and ecofriendly catalyst for chemoselective N-tert butyloxycarbonylation of amines under the solvent-free conditions
Ingale, Ajit P.,Shinde, Sandeep V.,Thorat, Nitin M.
, p. 2528 - 2543 (2021)
Sulfated tungstate catalyzed an efficient and ecofriendly protocol has been described for the chemoselective N-tert-butyloxycarbonylation of amines under the solvent-free conditions at room temperature. The variety of functionalized aliphatic, aromatic and heteroaromatic amines efficiently undergoes the N-tert-butyloxycarbonylation under the developed protocol. The aminoalcohol, aminophenol, aminoester as well as various chiral amines underwent the chemoselective N-Boc protection under the optimized reaction condition. The rapid reaction rate, mild conditions, very good functional group tolerance, excellent yield, solvent-free, easy recovery products and excellent catalyst recyclability are the advantages of this protocol. This makes the protocol feasible, economical and environmentally benign.
3-(ureido-methyl)-4-aryl-pyridine compound, preparation method thereof and application thereof as anti-hepatoma medicament
-
Paragraph 0071; 0072; 0075, (2018/03/26)
The invention discloses a 3-(ureido-methyl)-4-aryl-pyridine compound, a preparation method thereof and application thereof as an anti-hepatoma medicament. The invention discloses a compound shown as aformula I or a pharmacologically-acceptable salt, crystal form and solvate thereof, wherein X is O or S; n is an integer of 0 to 3; R1, R2, R3, R4 and R5 are independently selected from H, cyan, COOR11, alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, trifluoromethyl, amino, nitro, hydroxyl, mercapto or halogen; R11 is selected from H or alkyl having 1 to 4 carbon atoms. Meanwhile, the invention also discloses a preparation method of the compound shown as the formula I. The compound disclosed by the invention has lower median inhibitory concentration (IC50), and a very good inhibition function on hepatoma carcinoma cells; moreover, the preparation method of the compound disclosed by the invention is simple and convenient, and has the advantages of mild reaction condition, convenience in operation and control, low energy consumption, high yield and low cost, and can be suitable for industrial production. The formula I is shown in the description.