申请人:Leo Pharmaceutical Products Ltd. A/S (Lovens Kemiske Fabrik
公开号:US05401868A1
公开(公告)日:1995-03-28
The present invention relates to hitherto unknown intermediate of formula, in which R.sub.1 stands for hydrogen or a straight or branched aliphatic C.sub.1 -C.sub.20 carbon chain or an aryl or aralkyl group, aryl and "ar" meaning an aromatic or heterocyclic, 5- or 6-membered ring substituent containing 1 or 2 hetero atoms selected among O, S and N, R.sup.1 optionally being further substituted, and its chain being interrupted by hetero atoms like oxygen, or by carbonyl group(s); and R.sup.3 stands for hydrogen or C.sub.1 -C.sub.3 alkyl. The present intermediates can be used in a one step method for producing prodrugs of formula, where D-H =drug itself.
本发明涉及到迄今为止未知的一种中间体,其化学式为,其中R.sub.1代表氢或直链或支链的脂肪族C.sub.1-C.sub.20碳链或芳基或芳基烷基,芳基和“芳”表示含有1个或2个在O、S和N中选择的杂原子的芳香或杂环5-或6元环取代基,R.sup.1可选择进一步取代,其链被氧等杂原子或羰基打断;而R.sup.3代表氢或C.sub.1-C.sub.3烷基。这些中间体可以用于一步法制备化学式的前药,其中D-H=药物本身。