13534-99-1Relevant articles and documents
3-Substituted 2-isocyanopyridines as versatile convertible isocyanides for peptidomimetic design
Ballet, Steven,Elsocht, Mathias,Hollanders, Charlie,Jida, Mouhamad,Maes, Bert U. W.,Renders, Evelien,Van der Poorten, Olivier
, p. 6863 - 6866 (2021/07/19)
We report the use of 3-substituted 2-isocyanopyridines as convertible isocyanides in Ugi four-component reactions. TheN-(3-substituted pyridin-2-yl)amide Ugi products can be cleaved by amines, alcohols, and water with Zn(OAc)2as a catalyst. In addition, the applicability of the method was demonstrated in constrained di-/tripeptides bearing acid and base sensitive protective groups obtainedviaUgi-4CR post-condensation modifications.
Preparation method of 2-amino substituted six-membered nitrogen-containing heterocycle complex
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Paragraph 0067; 0068, (2019/02/08)
The invention discloses a preparation method of a 2-amino substituted six-membered nitrogen-containing heterocycle complex. The preparation method comprises the following steps: mix 2-fluorine substituted six-membered nitrogen-containing heterocycle complex and amidine hydrochloride salt compound, and then react under the action of a alkaline substance to obtain a 2-amino substituted six-memberednitrogen-containing heterocycle complex. Preferably, the 2-amino substituted six-membered nitrogen-containing heterocycle complex is a 2-amino pyridine compound, a 2-aminopyrimidine compound or a 2-aminopyrazine compound. Compared with the prior art, the method has the advantages of simple synthesis conditions, less reaction steps, mild reaction conditions, low cost of the catalyst used, less waste discharge and good functional group tolerance.
Preparation method of intermediate 3-bromopyridine-2-amine
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Paragraph 0037; 0039; 0040; 0041, (2017/03/17)
The invention relates to the field of medicinal chemistry, in particular to a preparation method of a phosphatidylinositol 3-kinase inhibitor intermediate. The preparation method of 3-bromopyridine-2-amine provided by the invention includes: taking 3-bromo-5-iodopyridine-2-amine as the starting raw material, carrying out halogen-metal exchange reaction, and conducting 5-position deiodination to obtain 3-bromopyridine-2-amine. The synthesis route of 3-bromopyridine-2-amine provided by the invention is different from the existing routes, and also has high yield of the product 3-bromopyridine-2-amine, thus being suitable for industrial production.