| abstract |
The invention belongs to the technical field of organic synthesis, in particular to an internal alkyne derivative and a preparation method thereof. The first aspect of the present application provides an internal alkyne derivative, the structural formula of the internal alkyne derivative is as shown in formula (I); wherein, R1 and R2 are independently selected from C1 ～C20 hydrocarbon groups, C5～C30 Aryl group or C5~C30 aromatic heterocyclic group, or silicon group such as triisopropylsilyl, dimethyl tert-butylsilyl, cyclohexyl-containing oxygen silicon ether. The preparation method of the present invention adopts the common and easy-to-obtain alkyl alcohol derivatives of formula (II) and the compound of formula (III) to realize the activation reaction based on saturated carbon-carbon of alkyl under the conditions of alkaline environment and oxidant, so as to obtain fast An efficient method for the construction of a variety of differently substituted internal alkyne derivatives. The preparation method of the present invention has simple and easy-to-obtain substrates, few reaction steps, simple operation, one-pot synthesis, and can realize efficient synthesis of various internal alkyne derivatives. |