Verfahren zum selektiven Phosphorylieren von Nukleosiden

摘要

1,151,948. Phosphorylation of nucleosides. ASAHI KASEI KOGYO K.K. 14 July, 1967 [14 July, 1966], No. 32628/67. Heading C2C. A process for converting the primary alcohol group of a nucleoside to the phosphate group comprises adding the nucleoside to a complex which comprises a phosphorus oxytrihalide, a carboxylic acid or an aqueous solution of a carboxylic acid, and an organic base, in a polar organic solvent medium, reacting them, and then mixing the resultant reaction mixture with water, and isolating the nucleotide. The phosphorus oxytrihalide, carboxylic acid or aqueous carboxylic acid, and organic base are preferably mixed in the molar proportion of 2-8: 1-4: 2-8, most preferably 2: 1: 2, and the reaction is preferably carried out at from- 30‹ to 30‹ C. Examples describe the preparation of disodium 51-inosinate, disodium 51-guanylate, 51-adenylic acid, disodium 51-cytidylate, disodium 51-uridinate, 1-α-D-arabinofuranosyl hypoxanthine-51-phosphate, 1-#-D-glucopyranosyl hypoxanthine 61-phosphate, and disodium 51- xanthylate.