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Acetohydrazone: A Transient Directing Group for Arylation of Unactivated C(sp3)-H Bonds
被引:93
|作者:
Ma, Fei
[1
]
Lei, Min
[2
]
Hu, Lihong
[1
,2
]
机构:
[1] E China Univ Sci & Technol, Shanghai Key Lab New Drug Design, Sch Pharm, Shanghai 200237, Peoples R China
[2] Chinese Acad Sci, Univ Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China
基金:
中国国家自然科学基金;
关键词:
INTRAMOLECULAR AMINATION;
POTENT INHIBITORS;
ACTIVATION;
DERIVATIVES;
INDOLINES;
OXIDATION;
ALCOHOLS;
RECEPTOR;
KETONE;
D O I:
10.1021/acs.orglett.6b01170
中图分类号:
O62 [有机化学];
学科分类号:
070303 ;
081704 ;
摘要:
A straightforward and efficient method has been developed for the synthesis of 2-benzylbenzaldehyde derivatives from 2-methylbenzaldehyde and iodobenzene via a C(sp(3))-H activation process. In the course of the activation reaction, acetohydrazone is formed between 2-benzylbenzaldehyde and acetohydrazine as a transient directing group. As a new kind of transient directing group, acetohydrazone exhibits a remarkable directing effect to give corresponding products in good to excellent yields.
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页码:2708 / 2711
页数:4
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