Practical preparation of 3,3-difluoropyrrolidine.
A practical and cost-effective synthesis of 3,3-difluoropyrrolidine is reported. The synthesis involves the isolation of two intermediates, which are prepared via two efficient through processes: (1) a Claisen rearrangement followed by a Ru(VIII)-catalyzed oxidation to prepare the 2,2-difluorosuccinic acid and (2) an efficient cyclization to form N-benzyl-3,3-difluoropyrrolidinone followed by BH(3).Me(2)S reduction.
Xu
Feng
F
Department of Process Research, Merck Research Laboratories, Rahway, NJ 07065, USA. feng_xu@merck.com
Simmons
Bryon
B
Armstrong
Joseph
J
Murry
Jerry
J