- Nitration of deactivated aromatic compounds via mechanochemical reaction
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A variety of deactivated arenes were nitrated to their corresponding nitro derivatives in excellent yields under high-speed ball milling condition using Fe(NO3)3·9H2O/P2O5 as nitrating reagent. A radical involved mechanism was proposed for this facial, eco-friendly, safe, and effective nitration reaction.
- Wu, Jian-Wei,Zhang, Pu,Guo, Zhi-Xin
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supporting information
(2021/05/05)
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- Synthesis method of 2-fluoro-3-nitrobenzoic acid intermediate raw material
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The invention discloses a synthesis method of a 2-fluoro-3-nitrobenzoic acid intermediate raw material. The invention provides a novel synthesis route, and an important medical intermediate can be rapidly and conveniently prepared from cheap and easily available raw materials. The process method comprises the following steps: starting from o-methylphenol, carrying out nitration reaction to selectively generate a key intermediate 2-methyl-6-nitrophenol, carrying out hydroxyl chlorination to generate 2-chloro-3-nitrotoluene, then carrying out fluorination reaction to generate 2-fluoro-3-nitrotoluene, and finally oxidizing methyl under the action of an oxidant to generate 2-fluoro-3-nitrobenzoic acid. The method is not only high in yield, but also suitable for large-scale production.
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- INHIBITING AGENTS FOR BRUTON'S TYROSINE KINASE
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Provided are compounds of Formula (I), or pharmaceutically acceptable salts thereof, methods for use as Bruton's tyrosine kinase and methods of production.
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Page/Page column 189-190
(2019/12/04)
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- Inexpensive NaX (X = I, Br, Cl) as a halogen donor in the practical Ag/Cu-mediated decarboxylative halogenation of aryl carboxylic acids under aerobic conditions
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Versatile and practical Ag/Cu-mediated decarboxylative halogenation between readily available aryl carboxylic acids and abundant NaX (X = I, Br, Cl) has been achieved under aerobic conditions in moderate to good yields. The halodecarboxylation is shown to be an effective strategy for S-containing heteroaromatic carboxylic acid and benzoic acids with nitro, chloro and methoxyl substituents at the ortho position. A gram-scale reaction and a three-step procedure to synthesize iniparib have been performed to evaluate the practicality of this protocol. A preliminary mechanistic investigation indicates that Cu plays a vital role and a radical pathway is involved in the transformation.
- Fu, Zhengjiang,Jiang, Ligao,Zuo, Qianming,Li, Zhaojie,Liu, Yanzhu,Wei, Zhenhong,Cai, Hu
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supporting information
p. 5416 - 5421
(2018/08/12)
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- Quinoline compound containing perfluoroalkyl substituent, as well as preparation method and application of quinoline compound
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The invention disclose a quinoline compound containing a perfluoroalkyl substituent, as shown in a general formula A-1, wherein the details of the definition of R2, R3, R4, R5, R6 and I are seen in the description. The invention further discloses a preparation method and application of the quinoline compound containing the perfluoroalkyl substituent. The quinoline compound containing the perfluoroalkyl substituent provided by the invention is suitable for agriculture insecticide.
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Paragraph 0095; 0096
(2017/02/17)
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- Silver-catalyzed decarboxylative halogenation of carboxylic acids
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Decarboxylative halogenation of carboxylic acids catalyzed by silver carbonate is reported. ortho-Nitrobenzoic acids react with copper(II) chloride or bromide in DMF/DMSO at 130-140 °C leading to the corresponding aryl halides in moderate to good yields.
- Luo, Yong,Pan, Xiaolin,Wu, Jie
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supporting information; experimental part
p. 6646 - 6648
(2011/02/21)
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- Process for the preparation of 2-chloro-4-nitro-alkylbenzene
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In the preparation of 2-chloro-4-nitro-alkylbenzene by reaction of 4-nitro-alkylbenzene with elemental chlorine or chlorine-releasing compounds in the presence of a Friedel-Crafts catalyst in the liquid phase, particularly high selectivities in respect of the target compounds chlorinated exclusively in the 2-position are achieved if a dibenzo-condensed sulphur heterocycle of the formula STR1 having the meanings given in the description for R1 to R8, X and n, is used as co-catalyst.
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