28458-89-1Relevant articles and documents
A complementary route to diaminopyrimidines through regioselective SNAr amination reactions
O'Donnell, Michael,Charrier, Jean-Damien
, p. 1515 - 1522 (2015)
A novel approach towards the production of diverse sets of diaminopyrimidines through sequential SNAr reactions is reported. The readily prepared 2-chloro-4-tetrafluorophenoxypyrymidine reacts regioselectively with amines at the C-2 position. The tetrafluorophenoxy at C-4 can then be replaced with amines in a second SNAr to afford easy access to a different and complementary set of diaminopyrimidines. The broad utility of this 'C-2 then C-4' two-step sequence has been demonstrated with a range of aromatic and aliphatic amines.
Synthesis method of aza-arylamine compound and aza-arylamine compound
-
Paragraph 0059; 0060; 0061; 0090, (2019/04/26)
The invention provides a synthesis method of an aza-arylamine compound as shown in a formula (I). The synthesis method comprises the following steps: an aza aromatic hydrocarbon compound as shown in aformula (II) reacts with an amine compound as shown in a formula (III) in presence of alkali and under a heating condition, so that u X substituent groups on an A ring of the compound as shown in theformula (II) are substituted by NRR in the compound as shown in the formula (III), and the compound as shown in the formula (I) is obtained, wherein A is an aza six-membered aromatic ring or five-membered aromatic ring, and is an independent single ring or is fused with a ring B; X refers to that the A ring has at least n X substituent groups, each X substituent group is independently selected from the group consisting of F, Cl, Br, I, CN, alkoxy of C and alkylthio of C, and n is a positive integer selected from 1-5; and the alkali is one or a mixture of more selected fromof BuOK, BuONa, BuONa, KHMDS, NaHMDS and LiHMDS. The synthesis method provided by the invention does not need the use of transition metal catalysts, is simple and convenient to operate, is economical and practical and is environmentally friendly. In addition, the invention also provides the aza-arylamine compound prepared by the method.
METHODS OF REGIOSELECTIVE SYNTHESIS OF 2,4-DISUBSTITUTED PYRIMIDINES
-
Paragraph 0292; 0293, (2015/04/15)
The present invention relates to the novel regioselective syntheses of 2,4-disubstituted pyrimidines through sequential nucleophilic aromatic substitutions.