KOTHARE MOHIT ATUL,BEAUCHAMPS MARIE GEORGES,ZHAO JINGJING,SAPIENZA JOHN,PAPA PATRICK,PYE PHILIP,KREILEIN MATTHEW MICHAEL,RIGGS JENNIFER,PACKARD GARRICK,MORTENSEN DEBORAH,JOKIEL PATRICK ANTHONY,PERRIN-
申请号：
NZ61813510
公开号：
NZ618135A
申请日:
2010.10.22
申请国别(地区):
NZ
年份:
2015
代理人:
摘要：
Disclosed is the use of compounds of formula (VII) such as sodium 2-(5-bromo-3-(ethylamino)pyrazin-2-ylamino)acetate as an intermediate in the preparation of compounds of formula (VIa) such as 7-bromo-1-ethyl-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one, the method comprising cyclising a compound of formula (VII) in the presence of a base or an acid, wherein said cyclisation occurs under conditions suitable to provide a compound of formula (VIa), wherein: R2 is H, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted heterocyclylalkyl, substituted or unsubstituted aralkyl, or substituted or unsubstituted cycloalkylalkyl； R3 is H, or a substituted or unsubstituted alkyl； Hal is a halogen； and R is the alkali metal salt of the carboxylate； wherein an alkyl group, unless the context requires otherwise, is a saturated, partially saturated, or unsaturated straight chain or branched non-cyclic hydrocarbon having from 1 to 10 carbon atoms； and a cycloalkyl group, unless the context requires otherwise, is a saturated or partially saturated cyclic alkyl group of from 3 to 10 carbon atoms having a single cyclic ring or multiple condensed or bridged rings, and wherein the method may further comprise preparing a compound having formula (II) (such as 7-(5-fluoro-2-methyl-4-(1H-1,2,4-triazol-3-yl)phenyl)-1-((trans-4-methoxycyclohexyl)methyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one), comprising contacting a compound of formula (VIa) with R1-Y in a solvent, in the presence of a palladium catalyst, wherein Y is B(OR+)2 or Sn(R++)3； R1 is substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted heterocyclylalkyl； and wherein the remaining substituents are as defined herein. Also disclosed is the compound sodium 2-(3,5-dibromopyrazin-2-ylamino)acetate which is
