123564-74-9Relevant academic research and scientific papers
Direct synthesis of guanidines using di(imidazole-1-yl)methanimine
Wu, Yong-Qian,Hamilton, Sean K.,Wilkinson, Douglas E.,Hamilton, Gregory S.
, p. 7553 - 7556 (2002)
A direct synthetic approach to guanidine compounds is reported here using di(imidazole-1-yl)methanimine and di(imidazole-1-yl)cyanomethanimine as guanylating reagents.
Aryl spiro compound containing formamidine as well as preparation method and application of aryl spiro compound
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Paragraph 0215, (2021/08/14)
The invention belongs to the field of medicinal chemistry, and particularly relates to an aryl spiro compound containing formamidine as well as a preparation method and application of the aryl spiro compound. The invention relates to three aryl spiro compounds as shown in general formulas I-III and pharmaceutically acceptable salts, enantiomers, non-isomers, tautomers, solvates, polymorphic substances or prodrugs thereof. On the basis that SHP099 is used as a lead compound, a brand new compound with guanidyl at the tail end is prepared, and the problems that an existing SHP2 inhibitor is single in structural framework and the like are solved. The aryl spiro compound has the important significance of providing many modification sites and providing a basis for later structural modification. Meanwhile, the embodiment of the invention proves that the compound has an allosteric inhibition effect on SHP2 phosphatase, and a skeleton support is provided for subsequent development of an SHP2 phosphatase inhibitor.
The synthesis of 2-amino-4(3H)-quinazolinones and related heterocycles via a mild electrocyclization of aryl guanidines
Sales, Zachary S.,Mani, Neelakandha S.,Allison, Brett D.
supporting information, p. 1623 - 1626 (2018/03/29)
A new method for the preparation of 2-amino-4(3H)-quinazolinones and similar fused heterocycles is described. Simply warming a mixture of an aryl guanidine and carbonyl diimidazole in acetonitrile results in formation of a putative N-amidinoisocyanate intermediate which undergoes a 6π-electron electrocyclic reaction with the aryl ring to generate the quinazolinone ring system. The mild conditions are compatible with a variety of functional groups, and the reaction is shown to be successful on multigram scale.
