Abstract The reactions of β??lapachone (1) with 1, 2??diaminoethane (2) and 1, 2?? diaminopropane (4) gave the tetracyclic pyrazine derivatives (3) and mixtures of (5) and (6), respectively, while reaction with o??phenylene diamine (7) gave the quinoxaline derivative (8). The structure of pyrazine derivative (3) is confirmed by single??crystal X??ray diffraction study.