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

作者：Yi Yun-Peng; Xu Wen-Jun; Huang Xin; Liang Jian-Ping; Shang Ruo-Feng^*

来源：Chinese Journal of Structural Chemistry, 2017, 36(9): 1433-1438.

DOI：10.14102/j.cnki.0254-5861.2011-1612

• pleuromutilin
• single-crystal structure
• antibacterial activities

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 P2(1)2(1)2(1) with a = 10.494(3), b = 16.997(5), c = 16.997 angstrom, Z = 4, D-c = 1.275 Mg.m(-3), mu = 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.

• 出版日期2017-9-15
• 单位兰州理工大学; 中国农业科学院