使用交叉偶联反应在位置2、4和7上进行吡咯并[3,2- d ]嘧啶骨架的C功能化。因此,2-(5-(苄氧基甲基)-2,4-二氯-5 H-吡咯并[3,2 - d ]嘧啶-7-基)乙醇是9-脱氮嘌呤和4,6-二氮杂吲哚的通用合成前体通过相应碘化物的乙烯基化,然后双键的氢硼化来制备α-己内酰胺。开发了抗病毒DHPA的9-(1,2-二羟乙基)-9-脱氮杂腺嘌呤(9-脱氮-1'-nor同类)的合成。另外,在吡咯并[3,2- d ]嘧啶支架的7位上的末端三键的甲基铝化中观察到异常的区域选择性,导致转化为(Z)-丙-1-烯。
[EN] COMPOSITIONS AND METHODS FOR INHIBITING VIRAL POLYMERASE<br/>[FR] COMPOSITIONS ET PROCÉDÉS D'INHIBITION D'UNE POLYMÉRASE VIRALE
申请人:BIOCRYST PHARM INC
公开号:WO2013158746A1
公开(公告)日:2013-10-24
Provided are compounds of Formula (I) as described herein. Compounds of Formula (I) are useful in methods of inhibiting viral RNA polymerase activity and viral replication. Also provided are pharmaceutical compositions comprising compounds of Formula (I), as well as methods of treating viral infections using compounds of Formula (I).
COMPOSITIONS AND METHODS FOR INHIBITING VIRAL POLYMERASE
申请人:Kotian Pravin L.
公开号:US20150191472A1
公开(公告)日:2015-07-09
Provided are compounds of Formula I:
as described herein. Compounds of Formula I are useful in methods of inhibiting viral RNA polymerase activity and viral replication. Also provided are pharmaceutical compositions comprising compounds of Formula I, as well as methods of treating viral infections using compounds of Formula I.