| abstract |
A useful process in the synthesis of compounds against picornavirus, which consists of: (a) performing the cyanomethylation of a compound of the formula V using bis (trimethylsyl) amide and bromoacetonitrile to produce a compound of the formula VI; <EMI FILE = "00063457_1" ID = "1" MFI = JPEG> (b) perform the decrease, then the cyclization, and then the deprotection of the compound of the formula VI to produce a compound of the formula VII; and <EMI FILE = "00063457_2" ID = "2" MFI = JPEG> (c) perform oxidation and olefination of the compound of formula VII by reacting the compound of formula VII with a complex of SO3-pyridine to produce a reaction mixture and react the reaction mixture with a compound for formula VIII to form a compound of formula IV: <EMI FILE = "00063457_3" ID = "3" IMF = JPEG> where R1 is H, F, a alkyl group, OR, SR, or an O-alkyl group, wherein each R41 is independently H or a lower alkyl; and X is any protective group accepted for nitrogen. The process of claim 1, wherein the compound of formula V is prepared from N-Boc L glutamic acid? -benzyl ester. The process of claim 1, wherein X is a Boc group. The process of affirmation 1, where R41 is H. The process of affirmation 1, where Z1 is H. The process of affirmation 1, where Z is -COOEt. |