Synthesis of aryl α,α-difluoroethyl thioethers a novel structure motif in organic chemistry, and extending to aryl α,α-difluoro oxyethers
作者:Ren Tomita、Nawaf Al-Maharik、Andrea Rodil、Michael Bühl、David O'Hagan
DOI:10.1039/c7ob02987j
日期:——
A method for the preparation of aryl α,α-difluoroethyl thioethers (ArSCF2CH3) is reported and the synthesis approach is extended to aryl α,α-difluoroethyl oxygen ethers. Selected building blocks are further elaborated in cross-coupling reactions and are incorporated into analogues of established trifluoromethyl ether drugs. Conformations are explored and log P studies of these motifs indicate that
报道了一种制备芳基α,α-二氟乙基硫醚(ArSCF 2 CH 3)的方法,并将合成方法扩展到芳基α,α-二氟乙基氧醚。在交叉偶联反应中进一步阐述了选定的结构单元,并将其并入已建立的三氟甲基醚药物的类似物中。对构象进行了探索,对这些基序的log P研究表明,它们的极性明显大于其三氟甲基醚类似物,从而使其对生物活性物质的发现具有吸引力。