An effective procedure for the acylation of azaindoles at C-3.
Conditions for attachment of acetyl chloride, benzoyl chloride, and chloromethyl oxalate to the 3-position of 4-, 5-, 6-, or 7-azaindoles were explored. Best results were achieved with an excess of AlCl(3) in CH(2)Cl(2) followed by the addition of an acyl chloride at room temperature.
Zhang
Zhongxing
Z
Department of Chemistry, The Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, Connecticut 06492, USA.
Yang
Zhong
Z
Wong
Henry
H
Zhu
Juliang
J
Meanwell
Nicholas A
NA
Kadow
John F
JF
Wang
Tao
T