《Table 1Optimization studies.a》

《Table 1Optimization studies.a》   提示:宽带有限、当前游客访问压缩模式
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《Co(Ⅲ)/Zn(Ⅱ)催化吲哚的分子内环丙烷化(英文)》


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a The reaction was carried out using 1a(0.2 mmol),2a(0.24 mmol),[Cp*Co(MeCN)3][SbF 6]2(5 mol%),and Zn(OAc)2(30 mol%)in DCM(2 mL)at30–45°C for 12–24 h.b Isolated yield.c Determined by 1H NMR.

We initiated our investigation by screening the reaction conditions of the coupling of N‐pyrimidinylindole(1a)with ene‐yne ketone(2a)under Co(III)/Zn(II)catalysis(Table 1).The preliminary experimentation highlighted the effectiveness of the combined Co(III)/Zn(II)catalysis.The control experi‐ments revealed that both Co(III)and Zn(II)were important for this transformation.The omission of Co(III)resulted in trace formation of the desired product(entries 1 and 3),whereas the exclusion of Zn(II)resulted in a lower yield(entries 2 and 4).Note that the transformation proceeded in a highly regioselec‐tive manner.Neither Co(III)nor Zn(II)is effective against de‐pression when applied alone(entries 1–4).The solvent was observed to exert a dramatic impact on the efficiency.Notably,dichloromethane was identified as the optimal solvent in terms of both the yield and diastereoselectivity,for the formation of3aa(entries 5–9).Lowering the reaction temperature further resulted in low efficiency(entry 10),and extending the reaction time resulted in a yield(entry 11)approximately equal to that under the optimized reaction conditions(entry 9).