899819-34-2

Upstream product

• 399-94-0 2-bromo-1,4-difluorobenzene 
• 920-39-8 isopropylmagnesium bromide 

Downstream Products

• 832152-08-6 (2S,3S)-1-chloro-2-(2,5-difluorophenyl)-3-methyl-4-pivaloyloxybutan-2-ol 
• 1146594-00-4 (2,5-difluorophenyl)cycloheptane 
• 1172623-96-9 (±)-tert-butyl (1-(2,5-difluorophenyl)-1-oxopent-4-yn-2-yl)carbamate 
• 241479-72-1 (2R,3R)-2-(2,5-difluoro-phenyl)-1-(1H-1,2,4-triazole-1-yl)butan-2,3-diol 
• 241479-73-2 (2R,3S)-2-(2,5-difluorophenyl)-3-methyl-2-[(1H-1,2,4-triazol-1-yl)-methyl]-oxirane 
• 241479-69-6 (2R)-2',5'-difluoro-2-(3,4,5,6-tetrahydro-2H-pyran-2-yloxy)-propiophenone 
• 1218935-59-1 (R)-(+)-2-(2,5-difluorophenyl)pyrrolidine 
• 1223404-90-7 (R)-5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)-3-nitropyrazolo[1,5-a]pyrimidine 

Relevant academic research and scientific papers

Synthetic method for antifungal drug intermediate (2R,3S)-1-(1,2,4-triazol)-2-difluorophenyl-2,3-epoxybutane

The invention discloses a synthetic method for an antifungal drug intermediate (2R,3S)-1-(1,2,4-triazol)-2-difluorophenyl-2,3-epoxybutane. The synthetic method comprises the following steps: (1) reacting a compound IV with a Grignard reagent to obtain a compound III; (2) employing a one-pot reaction to react the compound III with trimethylsulfoxonium iodide and 1,2,4-triazole and then react with p-toluenesulfonic acid, so as to obtain a compound II; and (3) reacting the compound II with methanesulfonyl chloride under an alkali condition to generate the target compound I, wherein the Grignard reagent is 2,4-difluorophenylmagnesium bromide or 2,5-difluorophenylmagnesium bromide, and the structural formula of the compound IV is shown in the specification. According to the synthetic route, the reaction conditions are mild and easy to control, the reaction route is simple, the related solvents in the reaction process all are common solvents, the reaction conversion rate is high, and the method possesses extremely high feasibility, is beneficial for industrialized batch production, and possesses extremely large exploitation potential and extremely good application prospect.

PROCESS FOR PRODUCING EPOXYTRIAZOLE COMPOUND AND INTERMEDIATE THEREFOR

The present invention provides a compound of the formula (I); wherein Ar represents difluorophenyl group, which is useful as an intermediate in a process for producing an epoxytriazole compound of the formula (VII); wherein Ar represents difluorophenyl group, which is a synthetic intermediate of antifungal agents. The present invention also provides a process for producing a compound of the formula (VII) which comprises epoxydation step, deprotection step, reaction step with a compound represented by RSO2X, and reaction step with 1,2,4-triazole; or comprises epoxydation step, reaction step with 1,2,4-triazole, deprotection step, reaction step with a compound represented by RSO2X and treatment step by a base.

Bromine-magnesium-exchange as a general tool for the preparation of polyfunctional aryl and heteroaryl magnesium-reagents

The scope of the Br-Mg-exchange reaction for the preparation of polyfunctional aryl and heteroaryl magnesium reagents has been studied. Various functional groups (ester, cyano, bromide) were tolerated in the exchange reaction allowing the preparation of polyfunctional Mg-reagents. Several dibromo- or tribromoheterocycles undergo a chemoselective mono-Br-Mg exchange leading to highly functionalized heterocycles.