| 摘要 |
PROBLEM TO BE SOLVED: To provide a synthesis method allowing for large-scale preparation of a phosphonate ester compound having high purity.SOLUTION: There is provided a morphic form of [[(S)-2-(4-amino-2-oxo-1(2H)-pyrimidinyl)-1-(hydroxymethyl)ethoxy]methyl]mono[3-(hexadecyloxy)propyl]ester (CMX001), characterized by an X-ray diffraction pattern including peaks at about 5.5 degree 2θ, 19.3 degree 2θ, 20.8 degree 2θ, and 21.3 degree 2θ. There is also provided the synthesis method comprising the steps (a) to (d): (a) adding (S)-trityl glycidyl ether to cytosine; (b) conducting etherification by phosphonic acid, P-[[[(4-methylphenyl)sulfonyl]oxy]methyl]-, mono[3-(hexadecyloxy)propyl]ester, and sodium salt; (c) removing a protecting-group; and (d) conducting recrystallization by a suitable organic solvent.SELECTED DRAWING: None |
