- Cobalt(II)-catalyzed regioselective C-H halogenation of anilides
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A cobalt-catalyzed regioselective C-H halogenation methodology is reported herein. The highlight of this work is the highly selective C-H functionalization of anilides, which results in high-yielding, versatile, and practical halogenated products. Thereby, brominations, chlorinations and iodinations of many electron-rich and electron-deficient anilides were achieved in a highly selective fashion. Mechanistic studies with respect to the pathway of the reaction are also described.
- Li, Ze-lin,Sun, Kang-kang,Cai, Chun
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supporting information
p. 5433 - 5440
(2018/08/12)
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- Synthesis method of important pharmaceutical and chemical intermediate 4-amino-3-chlorophenol
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The present invention discloses a synthesis method of important pharmaceutical and chemical intermediate 4-amino-3-chlorophenol, and the method comprises the following steps: acetylation of p-aminophenol, triethylamine and an acylating agent to obtain 4-acetamino phenyl acetate shown as a formula I; chlorination of the formula I compound and a chlorinated reagent to obtain 4-acetamino-3-phenyl chloroacetate shown as a formula II; and reaction of the formula II compound and an alkali at 80-120 DEG C to obtain the 4-amino-3-chlorophenol. The preparation method has the advantages of easy availability of raw materials, low cost, mild condition, high process operability and controllability, high yield and no need of complex post-treatment to obtain the high-purity 4-amino-3-chlorophenol.
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Paragraph 0033
(2017/08/29)
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- Novel Compounds
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The present invention relates to the new compounds of general formula I wherein A, U, V, X, Y, R1, R2 and R3 are defined as stated hereinafter, the tautomers, the isomers thereof, the diastereomers, the enantiomers, the hydrates, the mixtures and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, medicaments containing these compounds, their use and processes for preparing them.
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Page/Page column 74
(2012/04/18)
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- Direct acetoxylation and etherification of anilides using phenyliodine bis(trifluoroacetate)
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Treatment of various anilides with 1.5 equiv. of phenyliodine bis(trifluoroacetate) (PIFA) and 1.0 equiv. of BF3·OEt 2 in AcOH at room temperature afforded the corresponding para-acetoxylated products with high regioselectivity. In addition, this reaction could be expanded to the etherification of anilides. In the presence of 2.0 equiv. of PIFA and 2.0 equiv. of BF3·OEt2, the reaction of anilides with alcohols provided the corresponding para-etherified products in good yields. The Royal Society of Chemistry 2011.
- Liu, Huan,Wang, Xuemin,Gu, Yonghong
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experimental part
p. 1614 - 1620
(2011/04/22)
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