FULL PAPER
place to afford the product and regenerate the PC
(Figure 1a). Overall, this type of reaction only con-
Results and Discussion
sumes light energy (photons). Nevertheless, the photo- We chose quinoxalin-2(1H)-one (1a) and phenyldiazo-
catalyst-based sequence is photocatalyst-dependent and nium salt 2a as the model substrates to demonstrate
its success depends upon the compatibilities of the our concepts. Initially, the reaction was carried out
potentials of the substrate with PC (here, E(PC*/PC+.) under photochemical conditions using eosin Y as
compared with E (SubÀ ./Sub), and E(PC+./PC) vs E photocatalyst. As expected, the desired coupling
(Int2/Int1) ).
Organic electrochemistry has emerged as an effi-
product 3aa was isolated in a 65% yield (Table 1,
cient, green and environmentally friendly method, by
which to achieve the CÀ H bond functionalization.[5]
Given the inherent parallels that both electrosynthesis
and photoredox chemistry utilize electrons as reagents
to activate the substrate molecule, many organic trans-
formation have been translated from photoredox-
catalysed methodology to electrochemical processes
and vice versa.[6] This concept is illustrated in Fig-
ure 1b. The electrochemical reduction of a Sub
generates the corresponding SubÀ ., which converts to
an intermediate, Int1. If the electrochemical reaction is
carried out in an undivided cell, the Int1 may be
oxidized at the surface of the anode to form a second
intermediate, Int2, which then goes on to produce the
product. In this electrochemical process, only electric-
ity energy is consumed. One main advantage of the
electrochemistry strategy is that the potential of the
electrodes (anode and cathode) can be controlled by
the operator, rather than depending upon the potentials
accessible to the photocatalyst; the electrodes function
as the PC. In addition, workup, separation and
isolation is required to recycle PC, whereas the
electrode can simply be removed from solution.
Table 1. Optimization of the reaction conditions.[a]
entry deviation from standard conditions
yield
(%)[b]
1
2
3
4
eosin Y, DMSO, blue LEDs, N2
none
CH3CN, MeOH, DMF or DMA as solvent
CH3CN:DMF (5:1), MeOH:DMF (5:1) or
MeOH:DMSO (5:1) as solvent
no electricity
65[c]
84
17–44[d]
23–57[d]
5
6
7
8
0[e]
2 mA
6 mA
82[e]
76[e]
76
No external electrolyte
[a] Reaction conditions: 1a (0.2 mmol) and 2a (0.4 mmol) in
°
DMSO (3 mL), undivided cell, 25 C, current of 4 mA,
graphite felt and Ni plate cathode (working area: 1 cm2) and
constant current electrolysis (CCE) for 2.5 h, 1.88 F/mol.
[b] Yield determined by HPLC.
[c] Isolated yield.
[d] n-Bu4NClO4 (1.5 equiv.) was used as electrolyte.
[e] Et4NBF4 (1.5 equiv.) was used as electrolyte.
Arylation reactions are widely used in organic
synthesis to construct arylated compounds.[7] Photo-
catalyzed arylation of C(sp2)À H bonds has emerged as
a promising and useful strategy. It has been reported
that, by employing Ru,[8] and Ir[9]-based transition entry 1). With this result in mind, we chose to explore
metal photocatalysts, or an organic dye such as eosin the transformation electrochemically. Notably, without
Y,[10] under visible light irradiation, aryl diazonium current, the desired product was not detected (Table 1,
salts undergo a series of transformations with (hetero) entry 5). It was observed that the best results could be
arenes or alkenes to give arylated products (Figure 2a). obtained by conducting a constant current electrolysis
Based on these understanding, we envisioned that the at 4 mA/cm2 in an undivided cell equipped with a
photocatalyzed arylation of C(sp2)À H bonds might also graphite felt anode and a nickel plate cathode without
proceed electrochemically. This communication de- supporting electrolyte. Under these conditions, the
scribes our efforts and demonstrates for the first time desired product 3aa was obtained in an 84% yield
that electrochemical paired electrolysis is an alternative (Table 1, entry 2). Although the 2.0 equiv. phenyl-
to the visible light photoredox-based oxidation quench- diazonium salt was used, the biphenyl was not
ing approach (Figure 2b).
detected. Use of other solvents such as CH3CN,
MeOH, DMF and DMA provided 17%–44% yields of
3aa (Table 1, entry 3). The use of mixed solvent
systems did not improve the reaction efficiency
(Table 1, entry 4). The electrochemical arylation
proved insensitive to the choice of electrolyte, although
the use of Et4NBF4 provided a slightly improved yield
(72% vs 64%–71%; see SI Table S2 for details). It was
observed that the anode and cathode materials play an
important role (see SI Table S3 for details). In addition,
Figure 2. Arylation of C(sp2)À H bonds.
Adv. Synth. Catal. 2019, 361, 1–7
2
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