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Stereoselective Synthesis of 3-Aminoindan-1-ones and Subsequent Incorporation into HIV-1 Protease Inhibitors

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NIAID Data Ecosystem2026-03-06 收录
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https://figshare.com/articles/dataset/Stereoselective_Synthesis_of_3_Aminoindan_1_ones_and_Subsequent_Incorporation_into_HIV_1_Protease_Inhibitors/3239947
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A new method for the stereoselective synthesis of 3-aminoindan-1-ones from triflates of salicylic sulfinyl imines and ethylene glycol vinyl ether has been developed. The reaction sequence starts with a regioselective Heck reaction followed by stereoselective Lewis acid mediated annulation. Acidic cleavage of the sulfinamides produced pure (R)- and (S)-3-aminoindan-1-ones, which were successfully isolated and incorporated into active HIV-1 protease inhibitors.
创建时间:
2016-05-05
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