(R)-八氢吡嗪并[2,1-c][1,4]噁嗪

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: Prepared according to the method used in the preparation of (S)-4-(2-chloro-4-morpholin-4-yl-thieno[3,2-d]pyrimidin-6-ylmethyl)-3-isopropyl-piperazin-2-one using (R)-octahydro-pyrazino[2,1-c][1,4]oxazine in place of (S)-3-isopropyl-piperazin-2-one. The title compound was obtained as a pale yellow solid (57 mg, 62%). Prepared

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: To a solution of (R)-hexahydro-pyrazino[2,1-c][1,4]oxazin-4-one (60 mg, 0.39 mmol) in dioxane (5 mL) was added LiAlH4 (1.5 mL, 1M solution in THF). The resulting mixture was heated at 80° C. for 2.5 h before the addition of iPrOH (0.5 mL) followed by a saturated aqueous solution of Na2SO4 (3 mL). Further Na2SO4 was added and the resulting mixture filtered through celite, washing with EtOAc. The resulting residue was purified by NH2 column to give the title compound as an oil (40 mg, 73%). the resulting mixture filtered through celite washing with EtOAc The resulting residue was purified by NH2 column