科研之友
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摘要
A simple and efficient sequence for the preparation of 1-arylbenzo[c]thiophenes has been developed. Thus, 2-(chloromethyl)-phenyllithiums, generated by treating 2-(chloromethyl)phenyl bromides with butyllithium, are allowed to react with aromatic aldehydes to afford the corresponding diarylmethanol derivatives. These alcohols are oxidized with pyridinium chlorochromate (PCC) to give aryl[(2-chloromethyl)phenyl]-methanones, of which treatment with sodium hydrogensulfide gives 1-aryl-1,3dihydrobenzo[c]thiophen-1-ols. Dehydration of these crude alcohols to the desired products can be accomplished by the treatment with a catalytic amount of p-toluenesulfonic acid.
- 出版日期2017-9-1
