- A 3 - amino - 4 - chlorophenyl boronic acid [...] alcohol ester synthesis method (by machine translation)
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The invention relates to a 3 - amino - 4 - chlorophenyl boronic acid [...] alcohol ester synthesis method. Mainly solves the technical problem of improving its yield. The invention synthetic method comprises the following steps: in [1, 1' - double-(diphenyl phosphino) ferrocene] palladium dichloride under the catalytic action of, 5 - bromo - 2 - chloro nitrobenzene in 1, 4 - dioxane and duplex [...] borate reaction, to obtain compound 1; compound 1 in ethanol and water in the mixed solution and ammonium chloride, iron powder reaction, nitro is reduced to the amino, to produce the target compound 2. As the expensive medicine intermediate, 3 - amino - 4 - chlorophenyl boronic acid ester in [...] widely applied in the pharmaceutical industry. (by machine translation)
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Paragraph 0005; 0008-0010
(2018/03/01)
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- Synthesis of trimethylstannyl arylboronate compounds by sandmeyer-type transformations and their applications in chemoselective cross-coupling reactions
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A synthetic method based on Sandmeyer-type reactions to access both tin- and boron-substituted arenes from nitroaniline derivatives is described. This transformation can be applied to the synthesis of a series of functionalized trimethylstannyl arylboronates. In addition, the chemoselective reaction of the Stille and Suzuki-Miyaura cross-coupling reactions is explored, and a series of m- and p-terphenyl derivatives have been synthesized by conducting consecutive one-pot Stille and Suzuki-Miyaura cross-coupling reactions.
- Qiu, Di,Wang, Shuai,Tang, Shengbo,Meng, He,Jin, Liang,Mo, Fanyang,Zhang, Yan,Wang, Jianbo
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p. 1979 - 1988
(2014/04/03)
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- Synthesis of pinacol arylboronates from aromatic amines: A metal-free transformation
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A metal-free borylation process based on Sandmeyer-type transformation using arylamines derivatives as the substrates has been developed. Through optimization of the reaction conditions, this novel conversion can be successfully applied to a wide range of aromatic amines, affording borylation products in moderate to good yields. Various functionalized arylboronates, which are difficult to access by other methods, can be easily obtained with this metal-free transformation. Moreover, this transformation can be followed by Suzuki-Miyaura cross-coupling without purification of the borylation products, which enhances the practical usefulness of this method. A possible reaction mechanism involving radical species has been proposed.
- Qiu, Di,Jin, Liang,Zheng, Zhitong,Meng, He,Mo, Fanyang,Wang, Xi,Zhang, Yan,Wang, Jianbo
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p. 1923 - 1933
(2013/03/29)
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