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

作　　者：衣云鹏 续文君 黄鑫 梁剑平 尚若锋 

机构地区：[1]Key Laboratory of New Animal Drug Project of Gansu Province,Key Laboratory of Veterinary Pharmaceutical Development,Ministry of Agriculture,Institute of Husbandry and Pharmaceutical Sciences of CAAS [2]College of Life Science and Engineering,Lanzhou University of Technology

出　　处：《Chinese Journal of Structural Chemistry》2017年第9期1433-1438,共6页结构化学（英文）

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)

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.

关 键 词：pleuromutilin single-crystal structure antibacterial activities 

分 类 号：O626[理学—有机化学]