| 摘要 |
A process for preparing 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil, which is also known as MKC-442, is disclosed. The process comprises synthesizing an isopropyl ss-ketoester, such as ethyl-2-isopropyl-3-oxo-4-phenyl-butyrate, using any known method, including from benzyl cyanide and ethyl-2-bromo-3,3-dimethyl-propionate with activated zinc in a Reformatsky reaction. The ethyl-2-isopropyl-3-oxo-4-phenyl-butyrate is then condensed with thiourea in one of two ways. First, the ethyl-2-isopropyl-3-oxo-4-phenyl-butyrate is condensed with thiourea in a two-base system in the presence of a solvent. A second process for condensing the ethyl-2-isopropyl-3-oxo-4-phenyl-butyrate with thiourea is conducted in the presence of potassium t-butoxide to form a benzyl isopropyl thiouracil, which is desulfurized in process step (B). The benzyl isopropyl uracil resulting from either process is then alkoxyalkylated in process to form MKC-442. |
