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Various hexahydropyrazino[1,2-b]isoquinolines were synthesised as simplified saframycin analogues. Construction of this core proceeded through a tetrahydroisoquinoline synthesis followed by acylation/alkylation of the tetrahydroisoquinoline nitrogen and subsequent ring closure using various aliphatic and aromatic amines. The resulting piperazinones were reacted with LiAlH 4 or LiAlH(OEt) 3 to synthesise further analogues.

Synthesis of Hexahydropyrazino[1,2-b]isoquinolines as Simplified Saframycin Analogues