Liu Ying, Huang Jiaqi, Sun Zhudi, Deng Yupian, Qian Yuhao, Huang Qingchun, Cao Song
Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology (ECUST), Shanghai 200237, China.
Key Laboratory of Organofluorine Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai, 200032, China.
Org Biomol Chem. 2024 Jun 12;22(23):4641-4646. doi: 10.1039/d4ob00567h.
A novel two-step synthesis of β-trifluoromethyl primary amines from readily available α-(trifluoromethyl)styrenes and phthalimide is developed. The first step involves a hydroamination between α-(trifluoromethyl)styrenes and phthalimide (PhthNH) with the assistance of a base. Next, the hydrazinolysis of the resulting -(β-trifluoromethyl-β-arylethyl)phthalimides with hydrazine hydrate affords the desired -(β-trifluoromethyl-β-arylethyl)amines.
开发了一种由易得的α-(三氟甲基)苯乙烯和邻苯二甲酰亚胺两步合成β-三氟甲基伯胺的新方法。第一步是在碱的协助下，α-(三氟甲基)苯乙烯与邻苯二甲酰亚胺(PhthNH)进行氢胺化反应。接下来，用肼水合物对所得的-(β-三氟甲基-β-芳基乙基)邻苯二甲酰亚胺进行肼解反应，得到所需的-(β-三氟甲基-β-芳基乙基)胺。
