| abstract |
PURPOSE: To obtain the novel compd. for AIDS therapeutic medicine, etc., by aminating the alkaline metal salt of a specific thymidine compd. with hydroxylamine-O-sulfonic acid, etc., in a basic media, then converting the amino group to a substd. amino group. n CONSTITUTION: This compd. expressed by formula II where R 1 is the amino group (e.g.; 3'-azide-3-amino-3'-deoxytymidine, etc.) is obtd. by adding alkaline metal methanolate (e.g.; sodium methanolate, etc.) to the compd. e.g.; 3'-azide-3'- deoxythmidine, etc.) expressed by formula I (R 2 is azide, fluorine) to form an alkaline metal salt, then treating the same with hydroxylamine-O-sulfonic acid, O-arylhydroxylamine, O-(arylsulfonyl)-hydroxylamine, etc., in the basic medium. In some cases, the third position amino group of the compd. is converted to a group such as (substd.) alkylamino group, alkyl ureide or guanidino, by which the desired compd. is obtd. n COPYRIGHT: (C)1992,JPO |