- Benzosultam Synthesis by Gold(I)-Catalyzed Ammonium Formation/Nucleophilic Substitution
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The synthesis of benzosultams has been achieved through a gold(I)-catalyzed ammonium formation strategy. Starting from easily available N-(2-alkynyl)phenylsulfonyl azetidine derivatives, a cyclization reaction generated a spiroammonium gold intermediate t
- Pertschi, Romain,Weibel, Jean-Marc,Pale, Patrick,Blanc, Aurélien
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- COMPOSITIONS AND METHODS FOR MODULAR CONTROL OF BIOORTHOGONAL LIGATION
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The present invention provides a compound having the structure: Formula (I) wherein R1 is H or a protecting group; R2 and R3 are each independently H, halo, C1-C6 alkyl, C2-C6 al
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Page/Page column 59; 61-62
(2020/06/19)
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- Inexpensive multigram-scale synthesis of cyclic enamines and 3-N spirocyclopropyl systems
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Cyclic enamines are important synthons for many synthetic and pharmacological targets. Here, we report an inexpensive, catalyst-free, multigram-scale synthesis for cyclic enamines with exocyclic double bonds and four- to seven-membered rings. This strategy is more conducive to scale up, permissive of functionalization around the cyclic system, and less sensitive to the nature of the N-protecting group than previously-described methods for cyclic enamine synthesis. Further, we explore application of these enamines to the synthesis of highly-strained spirocyclic 3N-cyclopropyl scaffolds.
- Kumar, Pratik,Zainul, Omar,Laughlin, Scott T.
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p. 652 - 656
(2018/02/07)
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