TY - JOUR
T1 - A novel synthesis of imatinib and its intermediates
AU - Liu, Haiyan
AU - Xia, Wenpin
AU - Luo, Yu
AU - Lu, Wei
PY - 2010/8
Y1 - 2010/8
N2 - A convenient method has been developed for the synthesis of imatinib and two of its intermediates. N-(2-Methyl-5-nitrophenyl)-4-(3-pyridyl)-2-pyrimidin amine, obtained from 2-(methylsulfonyl)-4-(3-pyridyl)pyrimidine via nucleophilic substitution, was reduced by N2H4H2O/FeCl 3·6H2O/C in 92% yield. The resulting amine was condensed with 4-[(4-methylpiperazin-1-yl)methyl]benzoic acid dihydrochloride, which was prepared from 4-(chloromethyl)benzonitrile via substitution and hydrolysis reactions, to provide the final product imatinib in good yield and high purity.
AB - A convenient method has been developed for the synthesis of imatinib and two of its intermediates. N-(2-Methyl-5-nitrophenyl)-4-(3-pyridyl)-2-pyrimidin amine, obtained from 2-(methylsulfonyl)-4-(3-pyridyl)pyrimidine via nucleophilic substitution, was reduced by N2H4H2O/FeCl 3·6H2O/C in 92% yield. The resulting amine was condensed with 4-[(4-methylpiperazin-1-yl)methyl]benzoic acid dihydrochloride, which was prepared from 4-(chloromethyl)benzonitrile via substitution and hydrolysis reactions, to provide the final product imatinib in good yield and high purity.
KW - 2-(methylsulfonyl)pyrimidine derivatives
KW - 4-(chloromethyl) benzonitrile
KW - Imatinib
KW - Substitution
UR - https://www.scopus.com/pages/publications/78149412119
U2 - 10.1007/s00706-010-0334-0
DO - 10.1007/s00706-010-0334-0
M3 - 文章
AN - SCOPUS:78149412119
SN - 0026-9247
VL - 141
SP - 907
EP - 911
JO - Monatshefte fur Chemie
JF - Monatshefte fur Chemie
IS - 8
ER -