The second-generation XPhos palladium preformed catalyst-based C–N cross-coupling through Buchwald–Hartwig amination with primary and secondary amines towards functionalized benzoxazepino(7,6-b)quinolines is accounted for. The microwave irradiation in dioxane provided the desired highly functionalized oxazepino quinolines, 5, in high yield and purity from the corresponding 2-chloro-3-formyl quinolines, 1, via intermediate, 4, in a sequential cyclization/Buchwald amination strategy. Besides, functional group tolerance, low catalyst loading, microwave assistance, and a wide scope of reactions are the advantages. Compounds 5a, 5b, 5c, 5d, 5e, and 6j showed 50% inhibition in antioxidant potency, whereas compounds 5f, 5g, 5m, 6h, 6j, and 6k showed potent activity alongside 70% inhibition of alpha-amylase and 50% inhibition of alpha-glucosidase, respectively. The results were supported by molecular docking studies of the active compounds with acarvostatin as a standard drug for antidiabetic activity.

中文翻译：

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设计，合成和计算机模拟苯并氧杂庚啶（7,6-b）喹啉作为潜在的抗糖尿病药

第二代XPhos钯通过Buchwald-Hartwig胺与伯胺和仲胺的胺化反应，向功能化的苯并az庚啶（7,6-b）喹啉进行了基于催化剂的C-N交叉偶联。在二恶烷中进行微波辐照，通过顺序的环化/布赫瓦尔德胺化策略，通过中间体4从相应的2-氯-3-甲酰基喹啉1中以高收率和纯度提供了所需的高度官能化的恶嗪庚基喹啉5。此外，官能团耐受性，低催化剂负载，微波辅助和广泛的反应范围是优点。化合物5a，5b，5c，5d，5e，和6j表现出50％的抗氧化剂效能抑制作用，而化合物5f，5g，5m，6h，6j和6k表现出强大的活性，分别具有70％的α-淀粉酶抑制作用和50％的α-葡萄糖苷酶抑制作用。以阿伏他汀为抗糖尿病活性的标准药物对活性化合物进行分子对接研究，为研究结果提供了支持。