Process for the Synthesis of Highly Functionalized Racemic and Non-Racemic Piperidines

Patent Status: 

Patent Filed

Indian Patent Applicaton No: 

2403/DEL/2010

Date Filed: 

07.10.2010

Department: 

Patent Category: 

Overview: 

Process for the synthesis of highly functionalized piperidines in stereochemically pure forms.

Key Features: 

  • This patent describes an efficient process for the synthesis of 2,6-disubstituted piperidines in diastereo as well as enantiopure forms starting from simple precursors like substituted 1,3-dicarbonyl compounds and imines.
  • The process involves a domino-imino-aldol-aza-Michael reaction sequences, the two steps are being executed sequentially in a single pot operation to afford the corresponding piperidine products in very good chemical yields.

Applications: 

  • Piperidin ring systems are versatile subunits, found in many naturally occurring alkaloids and drug molecules.
  • Synthesis of a wide variety of drug like molecules having piperidine ring systems as the common structural element.

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