883715-40-0Relevant articles and documents
PERK INHIBITING COMPOUNDS
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Paragraph 0183-0184, (2021/03/05)
Provided herein are compounds of formula (I), compositions, and methods useful for inhibiting PERK and for treating related conditions, diseases, and disorders.
Synthesis of Amino- and Hydroxymethyl Benzoxaboroles: Prominent Scaffolds for Further Functionalization
Fuscaldo, Rodrigo S.,Vontobel, Pedro H. V.,Boeira, Eduam O.,Moro, Angélica V.,Costa, Jessie S. da
, p. 2050 - 2055 (2019/03/07)
Herein, we describe the development of a short, simple, and efficient synthesis of amino- and hydroxymethyl-substituted benzoxaboroles. The key step in our strategy was the early stage incorporation of the boron by the borylation of an aniline. The formed boronates were then elaborated to the final products in two additional steps, usually in good yields. The synthetic sequence was amenable to be performed on a preparative scale and 4-amino benzoxaborole 4b and 6-hydroxymethyl benzoxaborole 10c have been prepared, without any significant decrease in the overall yield. The amino and hydroxymethyl present at the molecules are useful for further elaboration and/or conjugation to bioactive molecules and therefore we believe that this method should be useful in the development of new compounds for Medicinal Chemistry.
Synthesis of trimethylstannyl arylboronate compounds by sandmeyer-type transformations and their applications in chemoselective cross-coupling reactions
Qiu, Di,Wang, Shuai,Tang, Shengbo,Meng, He,Jin, Liang,Mo, Fanyang,Zhang, Yan,Wang, Jianbo
, p. 1979 - 1988 (2014/04/03)
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.