A Simple Aliphatic Diamine Auxiliary for Palladium-Catalyzed Arylation of Unactivated <i>β</i>
-C(<i>sp</i>
<sup>3</sup>
)-H Bonds
作者:Jiang Lou、Quannan Wang、Yuan He、Zhengkun Yu
DOI:10.1002/adsc.201801022
日期:2018.12.3
Palladium‐catalyzed β‐C(sp3)‐Harylation of aliphatic acid derivatives was achieved by means of 2‐dimethylaminoethylamine auxiliary as a directing group. The β‐C(sp3)‐Harylation reactions with aryl and heteroaryl iodides efficiently afforded the corresponding arylated hydrocinnamic acid derivatives. Direct β‐C(sp3)‐H alkynylation, and arene C−H arylation and alkynylation were also realized under the
A drug having a high affinity for benzodiazepine ω
3
receptors and showing curative and preventive effects for anxiety and depression, which comprises as the active ingredient, for example, a compound of the formula (1):
wherein R
1
and R
2
are independently a hydrogen atom, an optionally substituted alkyl group, an optionally substituted aryl group, etc.,
R
3
and R
4
are independently a hydrogen atom, an optionally substituted alkyl group, etc.,
R
5
, R
6
, R
7
and R
8
are independently a hydrogen atom, an optionally substituted alkyl group, an optionally substituted aryl group, etc.,
X is an oxygen atom, a sulfur atom, NR
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, etc. (in which R
10
is a hydrogen atom, an optionally substituted alkyl group, etc.)