An Efficient Novel Synthesis of 14-O-[(4-Amino-6-hydroxy-pyrimidine-2-yl)thioacetyl] Mutilin and the

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The title structure of 14-O-[(4-amino-6-hydroxy-pyrimidine-2-yl)thioacetyl] mutilin, C_(26)H_(47)N_3O_5S, has been synthesized using 22-O-tosyl pleuromutilin and 4-amine-6-hydroxy-2-mercatopyrimidine monohydrate, and its structure was characterized by IR, NMR, H RMS and single-crystal X-ray diffraction. This compound has a 5-6-8 tricyclic carbon skeleton and a pyrimidine ring. It crystallizes in orthorhombic, space group P2_12_12_1 with a = 10.494(3), b = 16.997(5), c = 16.997 ?, Z = 4, D_c = 1.275 Mg×m~(–3), μ = 0.220 mm~(–1), F(000) = 1248, wR(F~2) = 0.1159 and R = 0.0381. The preliminary biological test showed that the title compound has more potent inhibitions to Staphylococcus aureus, MRSA and MRSE than that of tiamulin fumarate in vitro. The title structure of 14-O - [(4-amino-6-hydroxy-pyrimidine-2-yl) thioacetyl] mutilin, C 26 H 47 N 3 O 5S, has been synthesized using 22-O-tosyl pleuromutilin and 4 -amine-6-hydroxy-2-mercatopyrimidine monohydrate, and its structure was characterized by IR, NMR, H RMS and single-crystal X-ray diffraction. This compound has a 5-6-8 tricyclic carbon skeleton and a pyrimidine ring. It crystallizes in orthorhombic space group P2_12_12_1 with a = 10.494 (3), b = 16.997 (5), c = 16.997 ?, Z = 4, D_c = 1.275 Mg × m -3, μ = 0.220 mm ~ -1), F (000) = 1248, wR (F ~ 2) = 0.1159 and R = 0.0381. The preliminary biological test showed that the title compound has more potent inhibitions to Staphylococcus aureus, MRSA and MRSE than that of tiamulin fumarate in vitro
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