73087-44-2

Upstream product

• 6039-97-0 3H-thiazol-2-one 
• 100-39-0 benzyl bromide 
• 100-44-7 benzyl chloride 
• 288-47-1 1,3-thiazole 
• 21277-97-4 2-benzyl-2H-isothiazol-3-one 

Relevant academic research and scientific papers

Preparation method of 3-substituted-thiazol-2(3H)-one compound

The invention discloses a preparation method of a 3-substituted-thiazol-2(3H)-one compound. The preparation method sequentially comprises the following steps: performing a reaction on an acyl azide compound and 2,5-dihydroxy-1,4-dithiane in a solvent at 80 DEG C plus or minus 5 DEG C for 18-21h; adding an aqueous sulfuric acid solution into an obtained reaction solution, reacting while stirring, and then filtering to remove a solid; performing a rotary evaporation on a filtrate to remove the solvent, then adding water, extracting by using ethyl acetate, washing an obtained organic layer by using a saturated salt solution, drying, then performing a rotary evaporation to remove the ethyl acetate, and performing silica gel column chromatography on an obtained concentrate to obtain the 3-substituted-thiazol-2(3H)-one compound. By the preparation method, the condition is mild, the yield is high, the posttreatment is convenient, the pollution is less, used raw materials are easy to obtain, and a simple and easily-implemented method is provided for efficiently synthesizing the 3-substituted-thiazol-2(3H)-one compound.

Metal-free C(sp2)-H functionalization of azoles: K2CO3/I2-mediated oxidation, imination, and amination

The direct C2-H oxidation and imination of a wide variety of azoles was achieved by using a commercially available simple K2CO3/I2 reagent combination. The iodinated azole adduct, produced via the in situ generation of N-heterocyclic carbene, is the key intermediate for C2-H oxidation, imination, and amination of azoles. Significantly, these reactions proceed under mild conditions with high to excellent yields, are scalable to large quantity and exhibit a broad substrate scope. Interestingly, this direct C2-H imination method allowed us to access various pharmacologically active N6-alkyl or N6-aryl substituted benzimidazoquinazolinone scaffolds through intramolecular C-H imination in a sequential one-pot reaction.

New heterocyclic inputs for the povarov multicomponent reaction

Oxa-, thia- and imidazolones are reactive inputs as electron-rich olefin components in Povarov reactions. On interaction with anilines and aldehydes, these substrates afford the corresponding multicomponent adducts in a regioselective manner. Intramolecular processes are also explored. Post-condensation oxidation provides convenient access to a variety of fused quinoline derivatives. Georg Thieme Verlag Stuttgart ? New York.

ALKYLATION OF 2-HYDROXYBENZOTHIAZOLE SALTS

The alkylation reactions of 2-hydroxybenzothiazole salts with various alkyl halides afford the N-alkylated derivatives.With alkyl halides prone to molecular reactions, 2-hydroxybenzothiazole in the presence of silver carbonate, yields N- and O-alkylated p