86891-79-4Relevant articles and documents
Discovery and synthesis of cyclohexenyl derivatives as modulators of CC chemokine receptor 2 activity
Brown, Gregory D.,Shi, Qing,Delucca, George V.,Batt, Douglas G.,Galella, Michael A.,Cvijic, Mary-Ellen,Liu, Rui-Qin,Qiu, Feng,Zhao, Qihong,Barrish, Joel C.,Carter, Percy H.
, p. 662 - 666 (2016/01/09)
A novel cyclohexenyl series of CCR2 antagonists has been discovered. This series of small, rigid compounds exhibits submicromolar binding affinity for CCR2. Modification of the substituents on the cyclohexene ring led to the identification of potent CCR2 antagonists. Progress from initial lead 5 (IC50 = 700 nM) to (-)-38 (IC50 = 9.0 nM) is discussed.
Copper/silver-cocatalyzed conia-ene reaction of linear β-alkynic β-ketoesters
Deng, Chen-Liang,Song, Ren-Jie,Guo, Sheng-Mei,Wang, Zhi-Qiang,Li, Jin-Heng
, p. 5111 - 5114 (2008/03/27)
A novel and general copper/silver catalytic system has been developed for the Conia-ene intramolecular reaction of linear β-alkynic β-ketoesters. In the presence of (CuOTf)2·C 6H6 and AgSbF6 (or AgOAc), a variety of the linear β-alkynic β-ketoesters selectively underwent the Conia-ene intramolecular reaction in moderate to good yields.
Synthetic Studies Aimed at the Dolastanes. An Attempted A + C -> ABC Approach
Belmont, Daniel T.,Paquette, Leo A.
, p. 4102 - 4107 (2007/10/02)
The dolastanes are marine diterpenes whose molecular array of fused 6-7-5 alicyclic rings is distinctive.As part of a program directed toward the synthesis of representatives of these bioactive natural products, the possibility of elaborating their framework by intramolecular cyclization to form the central seven-membered ring has been examined.An expedient two-step route to keto ester 8 was developed.This intermediate proved receptive to copper-promoted conjugate addition of allylmagnesium bromide and lithium.The acetal 21 to be subsequently derived from these adducts could be conveniently crafted into the highly functionalized 2-cyclopentenones 27.Central to the synthetic strategy was the need for intramolecular C-C bond formation within 27.Because we were singularly unsuccessful in achieving the desired end result, this particular approach appears unsuited for gaining access to the dolastanes.
