- Modular Dual-Tasked C-H Methylation via the Catellani Strategy
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We report a dual-tasked methylation that is based on cooperative palladium/norbornene catalysis. Readily available (hetero)aryl halides (39 iodides and 4 bromides) and inexpensive MeOTs or trimethylphosphate are utilized as the substrates and methylating reagent, respectively. Six types of "ipso" terminations can modularly couple with this "ortho" C-H methylation to constitute a versatile methylation toolbox for preparing diversified methylated arenes. This toolbox features inexpensive methyl sources, excellent functional-group tolerance, simple reaction procedures, and scalability. Importantly, it can be uneventfully extended to isotope-labeled methylation by switching to the corresponding reagents CD3OTs or 13CH3OTs. Moreover, this toolbox can be applied to late-stage modification of biorelevant substrates with complete stereoretention. We believe these salient and practical features of our dual-tasked methylation toolbox will be welcomed by academic and industrial researchers.
- Gao, Qianwen,Shang, Yong,Song, Fuzhen,Ye, Jinxiang,Liu, Ze-Shui,Li, Lisha,Cheng, Hong-Gang,Zhou, Qianghui
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supporting information
p. 15986 - 15993
(2019/10/11)
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- Design and synthesis of potent amido- and benzyl-substituted cis-3-amino-4-(2-cyanopyrrolidide)pyrrolidinyl DPP-IV inhibitors
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The cis-3-amino-4-(2-cyanopyrrolidide)-pyrrolidine template has been shown to afford low nanomolar inhibitors of human DPP-IV that exhibit a robust PK/PD profile. An X-ray co-crystal structure of 5 confirmed the proposed mode of binding. The potent single
- Corbett,Dirico,Song,Boscoe,Doran,Boyer,Qiu,Ammirati,VanVolkenburg,McPherson,Parker,Cox
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p. 6707 - 6713
(2008/09/17)
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