Method for preparing Derivatives of 3,4 - dihidropirazin 2,3-b pirazin - 2 (1H) - One, intermediaries that Synthesis and Process for preparing them

摘要

Item 1: a method to prepare a formula compound (1),The method comprises contacting a compound of the formula (2) with R1-Y in a solvent, in the presence of a palladium catalyst, wherein said contact occurs under suitable conditions to provide a compound of the formula 1, wherein: X it is halogen, B (OR +) 2 or Sn (R ++) 3; Y is halogen, triflate, B (OR +) 2 or Sn (R ++) 3; where a) when X is halogen, then Y is B (OR +) 2 or Sn (R ++) 3; or b) when Y is halogen or triflate, then X is B (OR +) 2 or Sn (R ++) 3; wherein each R + is independently hydrogen or C1-3 substituted or unsubstituted alkyl, or each R +,In R1, c1-8 tar is replaced or not replaced, arilo is replaced or not replaced, cyclopropyl compound is replaced or not replaced, isocyclohexane is replaced or not replaced, or isocyclohexane is replaced or not replaced; R2 is h, c1-8 substituted or unsubstituted, cyclododecane substituted or unsubstituted, isocyclododecane substituted or unsubstituted, cyclododecane substituted or unsubstituted, cyclododecane substituted or unsubstituted, and R3 and R4 are h, respectively,C1-8: substituted or unsubstituted tar, substituted or unsubstituted arilo, substituted or unsubstituted cyclododecane, substituted or unsubstituted isocyclododecane, substituted or unsubstituted isocyclododecane, substituted or unsubstituted aralquilo, substituted or unsubstituted cyclododecalkylquilo, or R3 and R4, and the atoms to which they are attached, They form a substituted or unsubstituted cyclopentyl compound, or a substituted or unsubstituted isopropyl compound, or R2 and R3 and R4, together with the atoms to which they attach, form a substituted or unsubstituted isopropyl compound, provided that the compound is not 6 - (4-hydroxyphenyl) - 4 - (3-toluene) - 3, 4-dihydropyridyl [2, 3-B] Pyridine-2 (1H) - ona,6 - (4 - (1h-1,2,4-triazol-5-il) fenil) - 3 - (cyclohexilmethy) - 3,4-dihydroxypyridine-2 (1H) - ona, or (R) - 6 - (4 - (1h-1,2,4-triazol-5-il) fenil) - 3 - (cyclohexilmetyl) - 3,4-dihydropyridine-n [2,3-b] piracin-1h.