Pudnika, Linda; Domraceva, Ilona; Werner, Thomas; Zalubovskis, Raivis; Grandane, Aiga published the artcile< Base-Free Catalytic Wittig-/Cross-Coupling Reaction Sequence as Short Synthetic Strategy for the Preparation of Highly Functionalized Arylbenzoxepinones>, Electric Literature of 112-63-0, the main research area is bromo formylphenyl methylfumarate preparation phosphine catalyst Wittig reaction; bromobenzoxepinone carboxylate preparation phenylboronic acid Suzuki coupling reaction; tributyl phenylstannane bromobenzoxepinone carboxylate Stille coupling reaction; phenylbenzoxepinone carboxylate preparation antitumor SAR.
A short and efficient synthetic route towards benzoxepine containing scaffold, which enables late stage modification was developed. Namely, base-free catalytic Wittig reactions enabled the synthesis of bromobenzoxepinones from readily available starting materials. Subsequent, Suzuki-Miyaura and Stille reactions proved to be suitable methods to access a variety of benzoxepinone diaryl derivatives by late stage modification in only three steps. This three-step reaction sequence was suitable for high throughput applications and gives facile access to highly complex mol. structures, which are suitable for further functionalization. The antiproliferative properties of selected arylbenzoxepinones were tested in-vitro on monolayer tumor cell line A549. Notably, in this initial screening, these compounds were found to be active in the micromolar range.
Synthesis published new progress about Antitumor agents. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Electric Literature of 112-63-0.
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