- Pd-Catalysed direct C(sp2)-H fluorination of aromatic ketones: Concise access to anacetrapib
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The Pd-cataylsed direct ortho-C(sp2)-H fluorination of aromatic ketones has been developed for the first time. The reaction features good regioselectivity and simple operations, constituting an alternative shortcut to access fluorinated ketones. A concise synthesis of anacetrapib has also been achieved by using late-stage C-H fluorination as a key step.
- Wu, Qiuzi,Mao, Yang-Jie,Zhou, Kun,Wang, Shuang,Chen, Lei,Xu, Zhen-Yuan,Lou, Shao-Jie,Xu, Dan-Qian
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supporting information
p. 4544 - 4547
(2021/05/17)
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- Preparation method of 4-chloro-2-fluoro-5-nitroacetophenone
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The invention discloses a preparation method of 4-chloro-2-fluoro-5-nitroacetophenone, the preparation method is characterized in that m-fluoroaniline is taken as an initial raw material, and the 4-chloro-2-fluoro-5-nitroacetophenone is obtained through acetylation amino protection, Friedel-Crafts acylation reaction, hydrolysis reaction, Sandmeyer reaction and final nitration, and the preparationmethod has the advantages of easily available raw materials, low reaction condition requirement, few side reactions and high yield.
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Paragraph 0030-0032
(2020/01/25)
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- SUBSTITUTED TETRAHYDROCARBAZOLE AND CYCLOPENTANOINDOLE DERIVATIVES
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The present invention provides substituted tetrahydrocarbazole and cyclopentanoindole derivatives as antagonists of DP receptor, and as such are useful for the treatment of prostaglandin D2 mediated diseases such as rhinitis, asthma and nasal congestion.
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Page/Page column 23
(2010/02/12)
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- PYRIMIDINE DERIVATIVES AND HERBICIDES CONTAINING THE SAME
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The present invention provides a pyrimidine derivative represented by the formula: wherein R1p and R1q are the same or different, and each represents (1)hydrogen, (2)halogen, (3) a C1-6alkyl group which may be substituted or (4) a C1-6alkoxy group, and so on, R2 is halogen, a C1-6alkyl group, cyano group, and so on, Ar is a phenyl group which may be substituted or is a condensed hetero ring which may be substituted, which has excellent selective herbicidal activity, and a herbicide containing the derivative.
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