3874-54-2Relevant articles and documents
Preparation method of flupiperidinol
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Paragraph 0089; 0095; 0098; 0104, (2021/03/24)
The invention belongs to the technical field of medicine preparation, and particularly relates to a preparation method of flupiperidinol. The preparation method of the fluoropiperidinol, provided by the invention, comprises the following steps of providing 4-(4-chlorphenyl)-4-piperidinol of which the purity is 99% or above, providing 4-chloro-1-(4-fluorophenyl)butan-1-one of which the purity is more than 99%, mixing the 4-(4-chlorphenyl)-4-piperidinol, 4-chloro-1-(4-fluorophenyl)butan-1-one, an alkaline substance and a catalyst, and carrying out a first substitution reaction to obtain a crudeproduct, and mixing the crude product with an organic solvent, and sequentially carrying out reflux and crystallization to obtain the flupiperidinol. The flupiperidinol prepared according to the preparation method provided by the invention has relatively high yield and purity.
Mn-Enabled Radical-Based Alkyl-Alkyl Cross-Coupling Reaction from 4-Alkyl-1,4-dihydropyridines
Wang, Jie,Pang, Yu-Bo,Tao, Na,Zeng, Run-Sheng,Zhao, Yingsheng
, p. 15315 - 15322 (2019/11/19)
Highly efficient alkylation of β-chloro ketones and their derivatives was achieved by means of domino dehydrochlorination/Mn-enabled radical-based alkyl-alkyl cross-coupling reaction. In situ-generated α,β-unsaturated ketones and their analogues were identified as the reaction intermediates. Known bioactive compounds, such as melperone and azaperone, could be easily prepared from β-chloropropiophenone in two steps.
Palladium and visible-light mediated carbonylative Suzuki-Miyaura coupling of unactivated alkyl halides and aryl boronic acids
Roslin, Sara,Odell, Luke R.
supporting information, p. 6895 - 6898 (2017/07/10)
Herein, a simple and efficient method for the palladium-catalyzed carbonylation of aryl boronic acids with unactivated alkyl iodides and bromides under visible-light irradiation, ambient temperature and low CO-pressure is presented. Notably, the procedure uses readily available equipment and an inexpensive palladium catalyst to generate the key alkyl radical intermediate. These mild conditions enabled the synthesis of a range of functionalized aryl alkyl ketones including the antipsychotic drug, melperone.