A practical synthesis and spectroscopic study of new potentially biologically active S-lithocholic acid-substituted derivatives of 2-thiouracil

作者：Pospieszny Tomasz^*; Malecka Izabela; Paryzek Zdzislaw

来源：Tetrahedron Letters, 2010, 51(32): 4166-4169.

DOI：10.1016/j.tetlet.2010.05.094

Five new S-3 alpha-acetoxy-5 beta-lithocholic acid methyl ester-substituted derivatives of 2-thiouracil and 6-methyl-2-thiouracil have been prepared. 5-Morpholino-methyl-2-thiouracil, 5-piperidinomethyl-2-thiouracil, and 5-(4-methylpiperidino)methyl-2-thiouracil have been obtained via the Mannich reaction between 6-methyl-2-thiouracil, paraformaldehyde, and the cyclic secondary amines morpholine, piperdine, or 4-methylpiperidine in ethanol. The structures of the compounds were confirmed by spectral ((1)H NMR, (13)C NMR, and FT-IR) analyses and mass spectrometry. Estimation of the pharmacotherapeutic potential has been accomplished for the synthesized compounds on the basis of Prediction of Activity Spectra for Substances (PASS).

• 出版日期2010-8-11