41270-71-7

Upstream product

• 854699-15-3 3-amino-5,6-diphenyl-pyrazine-2-carboxylic acid 
• 41270-66-0 2-chloro-5,6-diphenylpyrazine 
• 76849-26-8 2-azido-5,6-diphenylpyrazine 
• 14892-98-9 6,7-diphenylpteridine-2,4(1H,3H)-dione 
• 1689-71-0 2,3-diphenyloxirane 
• 69816-37-1 2-amino-acetamidine dihydrobromide 
• 18591-57-6 5,6-diphenyl-2-hydroxypyrazine 

Downstream Products

• 190440-48-3 1-Benzoyl-3-(5,6-diphenyl-pyrazin-2-yl)-thiourea 

Relevant academic research and scientific papers

Synthesis method of selexipag intermediate

The invention relates to the technical field of medicine synthesis, in particular to a synthesis method of a selexipag intermediate. The preparation method comprises the following steps: reacting a compound as shown in a formula III with 2-aminoacetamidine hydrobromide under the action of a catalyst to obtain a compound as shown in a formula IV; reacting the compound as shown in the formula IV with 4-bromo-1-butanol under the action of alkali to obtain a compound as shown in a formula V; and carrying out N-alkylation reaction on the compound as shown in the formula V under the action of alkali to obtain the selexipag intermediate as shown in the formula I: 4-[(5, 6-diphenylpyrazine-2-yl) (isopropyl alcohol group) amino]-1-butanol. The invention creates a novel synthesis method of the selexipag intermediate, and the method has the advantages of cheap and easily available raw materials, simple operation, mild conditions and high yield.

Studies on pyrazines; part 30: Synthesis of aminopyrazines from azidopyrazines

Azidopyrazines do not undergo reduction by reagents that are effective for the preparation of alkyl- or arylamines from the azides because the heterocyclic azides exist in the bicyclic form of tetrazolo[1,5-a]pyrazines. Nevertheless, the conversion into aminopyrazines was achieved by hydrogenolysis in the presence of ammonium hydroxide and palladium-on-carbon or particularly by reduction with tin(II) chloride in methanolic hydrochloric acid, in 34-87% yields. To elucidate the successful progress of the reaction, the equilibrium of azide-atetrazole was examined by 1H NMR spectroscopy in various solvents.

A SIMPLE METHOD FOR THE PREPARATION OF SOME AMINO N-HETEROAROMATICS

The heating of some halogenated pyrazines, pyridines, and quinolines with benzamide in the presence of potassium carbonate gave the corresponding amino derivatives.The similar reaction using acetamide afforded acetamido derivatives, together with amines in some cases.