- One-Pot C-H Arylation/Lactamization Cascade Reaction of Free Benzylamines
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An efficient method has been developed for the synthesis of seven-membered biaryl lactams involving Pd-catalyzed, native amine-directed, ortho-arylation of benzylamines followed by in situ lactamization. This cascade sequence is enabled by the use of 2-iodobenzoates, which facilitates C-H arylation from the free amine under conditions that typically require an improved directing group approach. This reaction is characterized by a broad substrate scope with good functional group tolerance. The need for an ester versus carboxylic acid-functionalized coupling partner is also explored, as is the potential for synthesizing eight-membered biaryl lactams. Various applications are also investigated, including access to the aza-brassinolide core.
- Chand-Thakuri, Pratibha,Landge, Vinod G.,Kapoor, Mohit,Young, Michael C.
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p. 6626 - 6644
(2020/07/14)
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- BISAMID-ZINKBASEN
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The present invention relates to zinc amide bases of the general formula (I) [in-line-formulae](R1R2N)2—Zn.aMgX12.bLiX2??(I)[/in-line-formulae] wherein R1 and R2 are e
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Page/Page column 7-8
(2010/07/04)
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