- Metal-Free Photoinduced Transformation of Aryl Halides and Diketones into Aryl Ketones
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The acylation of aryl halides to prepare aryl ketones without metal catalyst represents an important yet challenging topic towards more sustainable ketone synthesis. Herein, we describe a simple and efficient metal-free protocol for the acylation of aryl halides with diketone under the irradiation of light utilizing N-methylpiperidine as base under an air atmosphere. This reaction can tolerate a wide range of functional groups and the corresponding ketones can be obtained in modest to good yields.
- Yao, Qiuli,Liu, Wenbo,Liu, Peng,Ren, Linjing,Fang, Xuehong,Li, Chao-Jun
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supporting information
p. 2721 - 2724
(2019/01/14)
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- Preparation method of velpatasvir intermediate
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The invention provides a preparation method of a velpatasvir intermediate. According to the preparation method, ortho-toluidine is taken as an initial raw material, amino acetylation protection, Friedel-Crafts acylation, deamination protection, diazotization, and bromination are adopted so as to obtain 3-bromomethyl-4-bromoacetophenone; and alkylation with 7-hydroxy-1-tetralone, intramolecular coupling, and bromination are adopted so as to obtain 9-bromo-3-(2-bromoacetyl)-10, 11-dihydro-5H-benzo[d]naphtho[2,3-b]pyran-8(9H)-one. The yield and the purity of the velpatasvir intermediate preparedvia the preparation method are high, cost is low, and large size production is convenient to realize.
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- METHOD OF FRIEDEL-CRAFTS ACYLATION OF ANILIDES
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An anilide is reacted with an acylating agent by using as a catalyst a tri (perfluoroalkane sulfonate) compound of any of the elements belonging to groups 3 to 5 and groups 13 to 15 in periods 4 to 6 of the periodic table, thereby bonding an acyl group to the benzene ring. Thus, ketoaniline derivatives, which are useful as physiologically active compounds or intermediates in synthesizing the same, are synthesized in high reaction yield by catalytic acylation.
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Page/Page column 6-7
(2008/06/13)
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