Background and overview[1]
Iodobenzene diethyl ester can be used as a pharmaceutical synthesis intermediate.
Application[1]
Examples of application of diethyl iodobenzene are as follows:
1) A method for hydrocarbon-activated acetoxylation of aryl groups using 2,1,3-benzothiadiazole as the directing group. The method is as follows: compound represented by raw material formula (I), acetic acid Palladium and diethyl iodobenzene are dissolved in a mixed solvent of acetic acid and acetic anhydride to obtain a reaction mixture. Under different reaction conditions, the obtained reaction mixture can produce a compound represented by formula (II) or a compound represented by formula (III). ; The reaction system of the method of the present invention is simple, and the solvent used is cheap and easy to obtain; the preparation of the substrate is simple and the yield is high, and the yield of the reaction of the present invention is good; the innovative point of the present invention is that under the action of the guiding group, the reaction can be carried out in one step 2,1,3-benzothiadiazole conjugated molecules are modified at specific points to introduce acetoxy groups, which greatly shortens the reaction route; the yield of the corresponding product obtained by the present invention is up to 99%;
2) Borane compounds used to prepare antibacterial treatments. The borane compounds are dodecaborane-substituted amides or dodecanoborane oxazoles. The preparation includes: (1) Monoamined dodecaborane Alkane is used as raw material, and under the action of sodium hydride, it is acylated with an acid chloride compound to obtain a dodecaborane-substituted amide; (2) The dodecaborane-substituted amide obtained in step (1) is dissolved in iodobenzene diethyl Oxidative coupling under the action of ester gives dodecanoxazole. The present invention also provides the application of the borane compound in the preparation of antibacterial drugs. The borane compound has extremely high antibacterial activity against certain Gram-negative bacteria and has great application prospects.
Main reference materials
[1] CN201810794062.2 Aryl hydrocarbon-activated acetoxylation method using 2,1,3-benzothiadiazole as the directing group
[2] CN201710612777.7 Borane compounds that can be used for antibacterial treatment and their preparation methods