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Difluoro-Substituted Bicyclo[1.1.1]pentanes for Medicinal Chemistry: Design, Synthesis, and Characterization.
Bychek, Roman M; Hutskalova, Valeriia; Bas, Yuliya P; Zaporozhets, Olga A; Zozulya, Sergey; Levterov, Vadym V; Mykhailiuk, Pavel K.
Afiliação
  • Bychek RM; Enamine Ltd. , Chervonotkatska 78 , Kyiv 02094 , Ukraine.
  • Hutskalova V; Enamine Ltd. , Chervonotkatska 78 , Kyiv 02094 , Ukraine.
  • Bas YP; Taras Shevchenko National University of Kyiv , Chemistry Department , Volodymyrska 64 , Kyiv 01601 , Ukraine.
  • Zaporozhets OA; Taras Shevchenko National University of Kyiv , Chemistry Department , Volodymyrska 64 , Kyiv 01601 , Ukraine.
  • Zozulya S; Taras Shevchenko National University of Kyiv , Chemistry Department , Volodymyrska 64 , Kyiv 01601 , Ukraine.
  • Levterov VV; Enamine Ltd. , Chervonotkatska 78 , Kyiv 02094 , Ukraine.
  • Mykhailiuk PK; Bienta , Chervonotkatska 78 , Kyiv 02094 , Ukraine.
J Org Chem ; 84(23): 15106-15117, 2019 12 06.
Article em En | MEDLINE | ID: mdl-31553875
ABSTRACT
A practical synthetic approach to the difluoro-substituted bicyclo[1.1.1]pentanes was developed. The key step was an addition of difluorocarbene (CF2) to electron-rich bicyclo[1.1.0]butanes by the CF3TMS/NaI system. The obtained difluoro-bicyclo[1.1.1]pentanes are suggested to be used as saturated bioisosteres of benzene rings for the purpose of drug discovery projects.

Texto completo: 1 Base de dados: MEDLINE Idioma: En Ano de publicação: 2019 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Idioma: En Ano de publicação: 2019 Tipo de documento: Article