The fluorination of 6-substituted 2-aminopyrazines with Selectfluor in the presence of Ag2CO3 is established under mild conditions. This method selectively produced the fluorinated 2-aminopyrazine derivatives in fair to high yield. The regioselectivity of this reaction strongly depends upon the substituent on the 2-aminopyrazines. The transformation of the fluorinated 2-aminopyrazine 3 h into a bioactive
在温和条件下建立了在Ag 2 CO 3存在下用Selectfluor进行6位取代的2-氨基吡嗪的氟化。该方法以中等至高收率选择性地生产氟化的2-氨基吡嗪衍生物。该反应的区域选择性在很大程度上取决于2-氨基吡嗪上的取代基。还讨论了氟化的2-氨基吡嗪3小时向生物活性化合物的转化。
TRIAZOLOPYRAZINE DERIVATIVES
申请人:Merck Patent GmbH
公开号:US20150051202A1
公开(公告)日:2015-02-19
Compounds of the formula I
in which R
1
, R
2
and R
4
have the meanings indicated in Claim
1,
are inhibitors of GCN2, and can be employed, inter alia, for the treatment of cancer.
[EN] TRIAZOLOPYRAZINE DERIVATIVES<br/>[FR] DÉRIVÉS DE TRIAZOLOPYRAZINE
申请人:MERCK PATENT GMBH
公开号:WO2013131609A1
公开(公告)日:2013-09-12
Compounds of the formula (I) in which R1, R2 and R4 have the meanings indicated in Claim 1, are inhibitors of GCN2, and can be employed, inter alia, for the treatment of cancer.