An efficient procedure for N-alkylation of pyrimidines and purines in the presence of tetra-n-butylammonium hydroxide（TBAH） is described. The method is very practical and the alkylation can occur at room temperature and the yields of the N-alkyl pyrimidines and purines were found to be excellent.
ZHANG Zhi-li~ , ZHOU Shou-xin, WANG Xiao-wei, WANG Hong-tao, CHEN Yan-li and LIU Jun-yi Department of Chemical Biology, School of Pharmaceutical Sciences
Methyluracil and 5-nitro-6-methyluracil react with variable molar quantities of benzoyl chloride in acetonitrile-pyridine at room temperature to give 1-N, 3-N-dibenzoyl-6- methyluracil 3b and 1-N-benzoyl-5-nitro-6-methyluracil 4b. The reactive rates of debenzoylation of 3b and 4b were investigated.
Aim To investigate the alkylation of 2-thiopyrimidine. Methods Treating the starting material 2-thiopyrimidine with chloromethyl ethers via a procedure of K2CO3 in DMF or with alkyl halide in CH3ONa-CH3OH at room temperature, to obtain the corresponding regioselective 2-S-allkyl pyrimidines. The products were determined by JH NMR, 2D NMR, IR and MS spectra. Results 2-S-alkyl-pyrimidines were regioselectively synthesized. Conclusion In different conditions with different alkyl halides, 2- thiouracil could be converted into the corresponding 2-S-alkylpyrimidines regioselectively.
＜正＞ The reverse transcriptase of HIV provides a key target for the development of anti-AIDS drugs. The discove...
WANG, Xiao-Wei ZHANG, Zhi-Li HAN, Peng MA, Xiao-Yan LIU, Jun-Yi( Department of Chemical Biology, School of Pharmaceutical Sciences , Peking University, Beijing 100083)
The reverse transcriptase of HIV provides a key target for the development of anti-AIDS drugs.The discovery of 1-[2-hydroxyethoxymethyl]-6-phenylthio-thymine(HEPT)as a compound with potent and selective in vivo activity against HIV-1[1]has led to the synthesis many new non-nucleoside reverse transcriptase inhibitors.
WANG Xiao-WeiZHANG Zhi-LiHAN PengMA Xiao-YanLIU Jun-Yi
Cobalamin-dependent methionine synthase plays a crucial role in folate metabolism and such would appear to be an excellent target for rational antifolate drug design. However, to date, no anticancer agents directed at this enzyme are available, but the enzyme is efficiently and specifically inhibited by N2O and this has proven invaluable for evaluating the biochemical consequence of enzyme inhibition and for mechanistic studies. [1,2] 2,5-Diamino-4-oxo-6-(3-butenyl) pyrimidine, a key intermediate in synthetic inhibitors of methionine synthase, was first synthesized using γbutenyl-β-ketoester and guanidine carbonate (Scheme 1). [3]……
ZHANG Zhi-Li WANG Hong-Tao WANG Xiao-Wei MA Xiao-Yan LIU Jun-Yi R.J. Griff B.T. Golding
