Synthesis of 2-indolyl methanamine derivatives catalyzed by diphenyl phosphate
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O621.3

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    Abstract:

    Friedel-Crafts reaction of 3-methylindoles and imines catalyzed by diphenyl phosphate can be used to synthesize 2-indolyl methanamines in one step, which has a wide range of pharmacological activities. The reaction conditions were optimized and the optimal reaction conditions were obtained as follows: n (3-methylindoles) ∶ n (imines) ∶ n(diphenyl phosphate) = 1.0 : 2.0∶0.1, the amount diphenyl phosphate is 0.0025 mmol, 1 mL anhydrous dichloromethane as solvent, room temperature, reaction time 0.5 h. 2-indolyl methanamine derivatives can be obtained in good yields (85~90%). The structures of the products were confirmed by 1HNMR, 13CNMR and HRMS.

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History
  • Received:January 22,2021
  • Revised:March 12,2021
  • Adopted:March 15,2021
  • Online: July 13,2021
  • Published: