摘要
The title structure of 14-O-[（4-amino-6-hydroxy-pyrimidine-2-yl）thioacetyl] mutilin, C26H47N3O5S, 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 P212121 with a = 10.494（3）, b = 16.997（5）, c = 16.997 A, Z = 4, Dc = 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, C26H47N3O5S, 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 P212121 with a = 10.494（3）, b = 16.997（5）, c = 16.997 A, Z = 4, Dc = 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.
基金
Supported by Basic Scientific Research Funds in Central Agricultural Scientific Research Institutions(No.1610322016007)
National Key Technology Support Program(No.2015BAD11B02)
Agricultural Science and Technology Innovation Program(ASTIP,No.CAASASTIP-2014-LIHPS-04)
