Tetrahedron Letters
Carbon–carbon bond formation via benzoyl umpolung attained
by photoinduced electron-transfer with benzimidazolines
b
a
b
Tomohito Igarashi a, , Eiji Tayama , Hajime Iwamoto , Eietsu Hasegawa
⇑
a Fundamental Sciences, Graduate School of Science and Technology, Niigata University, 8050, Ikarashi 2-no-cho, Nishi-ku, Niigata 950-2181, Japan
b Department of Chemistry, Faculty of Science, Niigata University, 8050, Ikarashi 2-no-cho, Nishi-ku, Niigata 950-2181, Japan
a r t i c l e i n f o
a b s t r a c t
Article history:
A photoreaction between benzoyl compounds, such as benzoylformate derivatives, and 2-(p-anisyl)-1,3-
Received 2 September 2013
Revised 2 October 2013
Accepted 7 October 2013
Available online 12 October 2013
dimethylbenzimidazoline in the presence of allyl bromide was found to give various allylated alcohols. In
the reaction of benzoylformates, a-hydroxy ester enolates, for which the negative charge occurs on the
carbonyl carbon of benzoyl (umpolung reactivity), are proposed to be generated as intermediates by elec-
tron-transfer from benzimidazolines to the photoexcited benzoylformates; these species react with allyl
bromide to produce a-allyl-a-hydroxy esters.
Keywords:
Ó 2013 Elsevier Ltd. All rights reserved.
2-Aryl-1,3-dimethylbenzimidazolines
Benzoylformates
Photoinduced electron-transfer
Umpolung reactivity
Carbon–carbon bond formation
Organic hydride donors, such as 1-benzyl-1,4-dihydronicotina-
mide,1,2 Hantzsch ester,3 9,10-dihydroacridine,2,4 and 1-acetyl-2,3-
dimethylimidazoline,5 are attractive research targets for chemists
and biochemists. 2-Aryl-1,3-dimethylbenzimidazolines (DMBI-H),
which also belong to this group of reagents, are known to reduce
olefins,6 ketones,7 organic halides,6–8 sulfones,7,8 cyclopropanes,8
and epoxy compounds.7,9 DMBI-H also acts as a hydrogen-storing
material, releasing hydrogen gas upon contact with Brønsted
acids.10
Previously, we reported that DMBI-H acts as an effective re-
agent to promote a photoinduced reduction of ketone A to produce
alcohol B (Scheme 1, Eq. 1).7g The reaction is proposed to generate
carbanion C, in which the carbonyl carbon becomes nucleophilic
(umpolung reactivity) and, finally, C captures a proton from water
to give B.
disclose the allylation of various benzoyl substrates by photoin-
duced electron-transfer with DMBI-H.
We conducted a photoreaction (k >280 nm, 500 W Hg–Xe lamp)
using benzophenone 1a and 2-(p-anisyl)-1,3-dimethylbenzimidaz-
oline 2a, capturing the resultant species in situ with allyl bromide
in acetonitrile at room temperature for 1 h. Then, a-allyl adduct 3a
was obtained in 54% yield (Table 1, entry 1). While the reaction of
benzaldehyde 1b gave 3b, albeit in low yield (entry 2), acetophe-
none 1c was inactive (entry 3). Notably, the reaction of methyl
benzoylformate 1d gave allylated mandelate 3d in good yield
Carbon–carbon (CꢀC) bond formations promoted by inversion
operators are well-established in organic synthesis.11 However, it
is difficult to construct a tertiary alcohol via umpolung reactivity;
one of the few examples is the SmI2 promoted CꢀC bond formation
of a
-keto esters/amides reported by Fukuzawa et al.12 We thought
that CꢀC bond formation would be possible when the appropriate
carbon electrophiles are captured by C in lieu of the protons sup-
plied by water (Scheme 1, Eq. 2). Formation of a quaternary carbon
via umpolung reactivity is unprecedented within the scope of pho-
toinduced electron-transfer reactions of DMBI-H. In this Letter, we
⇑
Corresponding author.
Scheme 1. The photo-reduction of
reactivity.
a benzophenone derivative via umpolung
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