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Chapter 1
Synthesis of functionalized pyrimidines
Figure-29
Atul R. Gholap et al. 60 has described the synthesis of 2-chloropyrimidine
derivatives from 2-hydroxypyrimidine derivatives using N,N-dimethylaniline and
POCl 3 as chlorinating agent under reflux condition (Figure-30).
Figure-30
Synthetic methods for the Suzuki-Miyaura coupling
The well known Suzuki reaction 61 is the organic reaction of an aryl or vinylboronicacid
with an aryl or vinyl-halide catalyzed by a palladium(0)complex forming
carbon-carbon bond. Some reported methods are described as under.
In 1981, Suzuki and Miyaura et al. have made a breakthrough in the
methodology for biaryl compounds using aryl boronicacids and aryl bromide under
homogeneous palladium catalyzed conditions in the presence of base 62 (Figure- 31).
Z
OH
Br B OH
3mol%Pd(Ph 3 ) 4
Aq. Na 2 CO 3
Benzene, refulx
Figure-31
Z
S. Li et al. 63 have synthesized Pd(OAc) 2 -catalyzed room temperature Suzuki
cross coupling reaction in aqueous media under aerobic conditions (Figure-32).
Figure-32
Y. M. A. Yamada et al. 64 have prepared highly active catalyst for the
heterogeneous Suzuki-Miyaura reaction by assembled complex of palladium and noncross
linked amphiphilic polymer (Figure-33).
Department of Chemistry, Saurashtra University, Rajkot-360005 15