“…Currently, spiro compounds are attracting attention as scaff olds in the search for modern drugs. [2][3][4][5][6][7][8][9] The combination of the intrinsic complexity and, more importantly, the rigidity of these scaff olds off er a number of advantages for programmed drug discovery.…”
A convenient synthesis of new 8-oxa-2-azaspiro[4.5]decane from commercially available reagents based on tetrahydropyran-4-carbonitrile and 1-bromo-2-fl uoroethane has been developed. This compound is promising for the production of important biologically active compounds.
“…Currently, spiro compounds are attracting attention as scaff olds in the search for modern drugs. [2][3][4][5][6][7][8][9] The combination of the intrinsic complexity and, more importantly, the rigidity of these scaff olds off er a number of advantages for programmed drug discovery.…”
A convenient synthesis of new 8-oxa-2-azaspiro[4.5]decane from commercially available reagents based on tetrahydropyran-4-carbonitrile and 1-bromo-2-fl uoroethane has been developed. This compound is promising for the production of important biologically active compounds.
An Au(I)-catalyzed cyclization/semipinacol rearrangement cascade of 1,6-enynes has been developed for the construction of spiro[4.5]decanes and 7-azaspiro[4.5]decanes. The use of JohnPho-sAuCl/NaBARF as a catalyst afforded functionalizable spirocyclic products with good diastereoselectivities of 6.7:1 to > 20:1 dr. A plausible reaction mechanism has also been proposed on the basis of previous literature and our experimental results.
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