A method for preparing (e)-propene-1-potassium trifluoroborate

Abstract

The invention discloses a novel method for preparing (E)-propylene-1-potassium trifluoroborate. The method specifically comprises steps as follows: 2,5-dimethyl-2,4-hexadiene and a borane tetrahydrofuran complex are taken as raw materials, iPP2BH (di (isopropylprenyl) borane) is prepared and is reduced through a formaldehyde solution after reacting with allylene so as to generate trimethyl borate, and then trimethyl borate reacts with a saturated water solution of KHF2 to generate (E)-propylene-1-potassium trifluoroborate. The preparation method has remarkable advantages as follows: the reaction raw materials are easy to acquire, the reaction operation is simple, the yield is high, the selectivity and the purity are good, and the production cost is low.

Description

technical field [0001] The invention relates to a new method for synthesizing a pharmaceutical intermediate organic boric acid derivative, belonging to the field of organic chemical synthesis, in particular to a method for preparing (E)-propene-1-potassium trifluoroborate. Background technique [0002] Organoboronic acid and its derivatives are an important class of pharmaceutical intermediates and organic chemical reagents, which are widely used in organic synthesis to form new C-C single bonds through Suzuki-Miyaura coupling reactions. Most organic boronic acids are stable at room temperature and can be stored for a long time, but some alkene or alkyne boronic acids are unstable at room temperature and are easy to deteriorate, which brings certain difficulties to the preservation of such boronic acids. If such boric acid is converted into boric acid derivatives such as boric acid ester and potassium trifluoroborate, its properties are stable and can be stored for a period ...

AI Technical Summary

Problems solved by technology

This method has a clean reaction, the yield is above 75%, and the selectivity of the reaction is good. It can generate 98% trans-olefin potassium borate. The only disadvantage of this method is that the price of the raw material dibromoborane dimethyl sulfide is too expensive, 1100RMB / 100mL (1M in CH 2 Cl 2 ), the cost of the reaction is too high, and the price of the target product generated is expensive, which is not suitable for large-scale industrial production

[0009] The above two known preparation methods all have expensive raw materials, are not easy to obtain, and the cost of the reaction is too high, which is not suitable for large-scale industrial production, which limits the mass production of the target product

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