Method for synthesizing chiral dihydro-6H-benzpyrole-[2,1-c][1,4]-benzodiazepine-6-ketone
A technology of benzodiazepine and indoline, applied in the synthesis of chiral dihydro-6H-indolo[2,1-c][1,4]-benzodiazepine-6-one It can solve the problems of no literature reports in synthetic research, and achieve the effect of chiral value-added, complete reaction, and simple reaction operation
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[0037] Example 1: Synthesis of various chiral dihydro-indolo[2,1-c][1,4]-benzodiazepin-6-ones by iridium-catalyzed asymmetric hydrogenation 2
[0038] In a nitrogen-filled glove box, (1,5-cyclooctadiene) iridium chloride dimer (0.0025 mmol, 1.7 mg) and chiral ligand (S, S, R)-C 3 *-TunePhos (0.0055 mmol) in the reaction bottle, add 1mL mixed solvent (the volume ratio of methylene chloride and toluene is 1: 2), stir at room temperature for 10 minutes, then transfer the prepared catalyst to another container containing Starting materials indolo[2,2-c][1,4]-benzodiazepine-6-one 1 (0.125 mmol) and morpholine trifluoroacetate (2.5 mg, 0.0125 mmol) In the reaction flask, 3 mL of mixed solvent (the volume ratio of dichloromethane and toluene is 1:2) is shared. The reaction bottle was placed in a stainless steel autoclave, and hydrogen gas was introduced at a pressure of 50 atmospheres, and the reaction was carried out at room temperature for 24 hours. Slowly release hydrogen, remov...
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