(New!!) N-alkylamidesとStyrenesのC-アルキル化とスケールアップ C-alkylation of N-alkylamides with Styrenes and Scale-up


Org. Biomol. Chem., 2018, 16, 7568-7573.

“C-alkylation of N-alkylamides with styrenes in air and scale-up using a microwave flow reactor”

Joshua P. Barham, Souma Tamaoki, Hiromichi Egami, Noriyuki Ohneda, Tadashi Okamoto, Hiromichi Odajima, and Yoshitaka Hamashima



  C-alkylation of N-alkylamides with styrenes is reported, proceeding in ambient air/moisture to give arylbutanamides and pharmaceutically-relevant scaffolds in excellent mass balance. Various amide and styrene derivatives were tolerated, rapidly affording molecular complexity in a single step; thus highlighting the future utility of this transformation in the synthetic chemistry toolbox. Reaction scalability (up to 65 g/h product) was demonstrated using a Microwave Flow reactor, as the first example of a C-alkylation reaction using styrenes in continuous flow.

実験結果提供:産業技術総合研究所 Joshua P. Barham先生、
静岡県立大学 濱島義隆先生、江上寛通先生
装置情報:200 mmキャビティ、200W