Synthetic process optimization of RDEA3170
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Key Project of Hubei Education Department(D20141510);Project of Hubei Education Department(B2017053)

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    Abstract:

    4-bromo-1-naphthonitrile was obtained by a new route of bromo-magnesium exchanging reaction, synthesis and dehydration of 4-bromo-1-naphthamide using 1,4-dibromonaphthalene as starting materials. The Miyaura borylation of 4-bromine-1- naphthonitrile and its Suzuki coupling with ethyl 2-(3-bromopyridine-4-yl)thio-2-methylpropionate were realized using Pd(PPh3)2Cl2 as catalyst by a continuous reaction method. The conditions for coupling reaction and the hydrolysis of the product to produce RDEA3170 were optimized. The overall yield of RDEA3170 is 42% and the optimized synthetic process is suitable for the industrial production.

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History
  • Received:May 05,2018
  • Revised:July 09,2018
  • Adopted:July 16,2018
  • Online: November 08,2018
  • Published:
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