Mild and General Conditions for Negishi Cross-Coupling Enabled by the Use of Palladacycle Precatalysts
作者:Yang Yang、Nathan J. Oldenhuis、Stephen L. Buchwald
DOI:10.1002/anie.201207750
日期:2013.1.7
A wide range of biaryls were synthesized by palladium‐catalyzed Negishi cross‐couplings at ambient temperature or with low catalyst loading. This protocol features the use of a recently reported aminobiphenyl palladacycleprecatalyst to generate the catalytically active XPhosPd0 species. Significantly, a wide range of challenging heterocyclic and polyfluorinated aromatic substrates can be employed
2-AMINOPYRIMIDIN-4-ONE AND 2-AMINOPYRIDINE DERIVATIVES BOTH HAVING BACE1-INHIBITING ACTIVITY
申请人:Yonezawa Shuji
公开号:US20110237576A1
公开(公告)日:2011-09-29
The present invention provides a compound which has an effect of inhibiting amyloid-β production and is useful as a therapeutic agent for diseases induced by production, secretion and/or deposition of amyloid-β proteins. The present invention relates to a compound represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof:
wherein A is optionally substituted carbocyclic diyl or optionally substituted heterocyclic diyl; B is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; R
1
is a group such as optionally substituted lower alkyl; R
2
is a group such as hydrogen; and R
3a
and R
3b
are each independently a group such as hydrogen, provided that the following compound is excluded.
Highly Efficient Monophosphine-Based Catalyst for the Palladium-Catalyzed Suzuki−Miyaura Reaction of Heteroaryl Halides and Heteroaryl Boronic Acids and Esters
作者:Kelvin Billingsley、Stephen L. Buchwald
DOI:10.1021/ja068577p
日期:2007.3.1
active and efficient catalyst system derived from a palladium precatalyst and monophosphine ligands 1 or 2 for the Suzuki-Miyaura cross-coupling reaction of heteroaryl boronic acids and esters has been developed. This method allows for the preparation of a wide variety of heterobiaryls in good to excellent yields and displays a high level of activity for the coupling of heteroaryl chlorides as well as