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

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(F2) =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.