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.