- Chemoselective Hydrosilylation of the α,β-Site Double Bond in α,β- And α,β,γ,δ-Unsaturated Ketones Catalyzed by Macrosteric Borane Promoted by Hexafluoro-2-propanol
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The B(C6F5)3-catalyzed chemoselective hydrosilylation of α,β- and α,β,γ,δ-unsaturated ketones into the corresponding non-symmetric ketones in mild reaction conditions is developed. Nearly 55 substrates including those bearing reducible functional groups such as alkynyl, alkenyl, cyano, and aromatic heterocycles are chemoselectively hydrosilylated in good to excellent yields. Isotope-labeling studies revealed that hexafluoro-2-propanol also served as a hydrogen source in the process.
- Zhan, Xiao-Yu,Zhang, Hua,Dong, Yu,Yang, Jian,He, Shuai,Shi, Zhi-Chuan,Tang, Lei,Wang, Ji-Yu
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p. 6578 - 6592
(2020/07/17)
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- Preparation methods of propafenone hydrochloride and intermediate 2'-hydroxydihydrochalcone thereof
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The invention discloses preparation methods of propafenone hydrochloride and an intermediate 2'-hydroxydihydrochalcone thereof. 2-phenyl-benzothiazoline is adopted as a reducing agent to construct a reduction system, carbon-carbon double bonds are reduced, double bonds in a substrate can be efficiently and selectively reduced, and the problem that the propafenone hydrochloride key intermediate 2'-hydroxydihydrochalcone is synthesized by using hydrogen is avoided. The used reducing agent is simple and easily available, and the preparation methods have the advantages of low requirements on reaction equipment and operation, suitableness for industrial production, no hydrogen and noble metals, safety and environmental friendliness.
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- Preparation of propafenone
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A process for the preparation of propafenone wherein 1. 2'-hydroxyacetophenone is reacted with epichlorohydrin, 2. the resulting 2-(2',3'-epoxypropoxy)-acetophenone is reacted with propylamine, 3. the resulting 2-(2'-hydroxy-3'-propylaminopropoxy)-acetophenone is reacted with benzaldehyde, accompanied by elimination of water, and 4. the resulting 2-(2'-hydroxy-3'-propylaminopropoxy)-benzalacetophenone is hydrogenated.
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