DOI: 10.1002/chem.201501811
Communication
&
Ate Complexes |Hot Paper|
Perfluoroalkyl and -aryl Zinc Ate Complexes: Generation,
Reactivity, and Synthetic Application
Xuan Wang,[a] Keiichi Hirano,*[a, b] Daisuke Kurauchi,[a] Hisano Kato,[a] Naoyuki Toriumi,[a]
Ryo Takita,[b] and Masanobu Uchiyama*[a, b]
In memory of Prof. Dr. Manfred Schlosser
Abstract: A combination of dimethylzinc, perfluoroalkyl
iodide, and LiCl afforded a new type of perfluoroalkyl (RF)
zinc ate complex. These complexes show much greater
thermal stability than conventional perfluorinated metal
species, such as RF–lithium species and Grignard reagents,
and they can be used at room temperature or higher. The
results of DFT calculations on the origin of the enhanced
stability are reported and the synthetic utility of RF-zincate
complexes is demonstrated.
Fluoroalkyl and -aryl motifs[1] are found in biologically impor-
tant[2] as well as functional materials.[3] Although numerous
Scheme 1. Perfluoroalkyl organometallic species.
synthetic methods for the installation of fluorine atoms into or-
ganic molecules have been developed over decades, the ma-
jority of them involve fluorination or trifluoromethylation.[4]
Perfluoroalkylation has attracted significantly less attention.[5–7]
Since the halogen–metal exchange reaction of organohalides
was pioneered by Gilman and Wittig,[8] generation methods
and synthetic applications of organolithium species and
Grignard reagents have been intensively investigated. Methods
for preparation of RF–Li and RF–MgX (Grignard reagents) by
halogen–metal exchange with perfluoroalkyl iodide (RF–I) in
combination with organolithium[9] or organomagnesium[10] re-
agents have also been established. However, these reagents
are very unstable and decompose via a- or b-elimination of
fluoride anion (Scheme 1). Consequently, these reagents can
be handled only at extremely low temperature and this limits
their practical application in synthetic organic chemistry.
fluoroalkylation, we started to examine the feasibility of achiev-
ing highly efficient and operationally benign perfluoroalkyla-
tion reactions by utilizing the high tunability of organozinc re-
agents.[12] Since Naumann and Lange reported that the halo-
gen–zinc exchange reaction proceeds between dialkylzinc and
RF–I and the resulting RF–Zn reagent is stable in the presence
of Lewis base(s),[13] this strategy was extensively adopted by
several research groups, including ours, to prepare and utilize
RF–Zn reagents.[14,15] Herein, we report the generation of RF–
zincate complexes by halogen–zinc exchange and demonstrate
their utility in organic synthesis.
In the initial screening to find suitable reagents, we pre-
pared various RF–organozinc reagents and assessed their reac-
tivity in the iodine–zinc exchange reaction with nonafluorobu-
tyl iodide at 08C, followed by in situ trapping with benzalde-
hyde at room temperature (Table 1). However, initial attempts
using various zincates, including mono-anionic zincates such
as Me3ZnLi (Table 1, entry 1) and di-anionic zincates such as
Me4ZnLi2 developed in our laboratory (entry 2),[11i] were unsuc-
cessful at room temperature, although at À788C 1a was ob-
tained in 73% and 62% yield, respectively. Gratifyingly, Me2Zn
prepared from ZnCl2 and 2 equivalents of MeLi afforded the
desired perfluoroalkylated product 1a in 62% yield without
any methylated byproduct formation (Table 1, entry 4), where-
as MeZnCl did not work (entry 3). The LiCl-free solution of
Me2Zn was totally unproductive (Table 1, entry 5). Addition of 2
equivalents of LiCl to the reaction of entry 3 gave 1a in 43%
yield (Table 1, entry 6).[16] Given Koszinowski’s reports[17] on the
formation of [Bu2ZnCl]Li as the sole species by complexation
of Bu2Zn with LiCl and our experimental results, we hypothe-
For over a decade, we have been working on organozincate
chemistry[11] and, given the paucity of general methods of per-
[a] Dr. X. Wang, Dr. K. Hirano, D. Kurauchi, H. Kato, N. Toriumi,
Prof. Dr. M. Uchiyama
Graduate School of Pharmaceutical Sciences
The University of Tokyo
7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033 (Japan)
[b] Dr. K. Hirano, Dr. R. Takita, Prof. Dr. M. Uchiyama
Advanced Elements Chemistry Research Team, RIKEN Center for Sustainable
Resource Science, and Elements Chemistry Laboratory, RIKEN
2-1 Hirosawa, Wako-shi, Saitama 351-0198 (Japan)
Supporting information for this article is available on the WWW under
Chem. Eur. J. 2015, 21, 10993 – 10996
10993
ꢀ 2015 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim