3999-69-7Relevant academic research and scientific papers
A Unified Catalytic Asymmetric (4+1) and (5+1) Annulation Strategy to Access Chiral Spirooxindole-Fused Oxacycles
Gao, Min,Gong, Xiangnan,Hu, Lin,Luo, Yanshu,Xia, Yuanzhi,Xu, Qianlan,Zhao, Yukun
supporting information, p. 19813 - 19820 (2021/08/03)
A unified catalytic asymmetric (N+1) (N=4, 5) annulation reaction of oxindoles with bifunctional peroxides has been achieved in the presence of a chiral phase-transfer catalyst (PTC). This general strategy utilizes peroxides as unique bielectrophilic four- or five-atom synthons to participate in the C?C and the subsequent umpolung C?O bond-forming reactions with one-carbon unit nucleophiles, thus providing a distinct method to access the valuable chiral spirooxindole-tetrahydrofurans and -tetrahydropyrans with good yields and high enantioselectivities under mild conditions. DFT calculations were performed to rationalize the origin of high enantioselectivity. The gram-scale syntheses and synthetic utility of the resultant products were also demonstrated.
Formal [5+1] annulation reactions of dielectrophilic peroxides: Facile access to functionalized dihydropyrans
Zhong, Chen,Yin, Qi,Zhao, Yukun,Li, Qinfeng,Hu, Lin
supporting information, p. 13189 - 13192 (2020/11/09)
A general [5+1] annulation reaction, which utilized 4-bromo- or 4-mesyloxy-but-2-enyl peroxides as unique five-atom bielectrophilic synthons to participate in the C-C and the subsequent umpolung C-O bond-forming reactions with C1 nucleophiles, has been developed for the facile synthesis of 2,2-disubstituted dihydropyrans in high yields under mild basic conditions. The dihydropyrans, which are readily prepared on a gram scale by this new method, can be flexibly transformed into the biologically important tetrahydropyrans and pyranones in 1-2 steps.
Synthesis of Novel Tetrahydroisoquinoline CXCR4 Antagonists with Rigidified Side-Chains
Jecs, Edgars,Miller, Eric J.,Wilson, Robert J.,Nguyen, Huy H.,Tahirovic, Yesim A.,Katzman, Brook M.,Truax, Valarie M.,Kim, Michelle B.,Kuo, Katie M.,Wang, Tao,Sum, Chi S.,Cvijic, Mary E.,Schroeder, Gretchen M.,Wilson, Lawrence J.,Liotta, Dennis C.
supporting information, p. 89 - 93 (2018/02/19)
A structure-activity relationship study of potent TIQ15-derived CXCR4 antagonists is reported. In this investigation, the TIQ15 side-chain was constrained to improve its drug properties. The cyclohexylamino congener 15a was found to be a potent CXCR4 inhi
Synthesis of 2-ene-1,4-diols by a new cascade-opening of 1,3-diepoxides: Towards an efficient synthesis of dihydroxytaxoid derivatives
Aldegunde, Maria J.,Castedo, Luis,Granja, Juan R.
supporting information; experimental part, p. 4785 - 4787 (2009/12/09)
The synthesis of dihydroxytaxoid derivatives, specially 2-Ene-1,4-diols using a new cascade-opening of 1,3-diepoxides was investigated. The study prepared a framework through a cascade ring-closing dienyne metathesis (RCDEYM) reaction from Dienyne. The me
Prostaglandin analogs
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, (2008/06/13)
Thromboxane receptor antagonist activity is exhibited by compounds of the formula STR1 wherein: V is --(CH 2) m --, --O--, or STR2 but if V is --O--or STR3 R 3 and R 4 must complete an aromatic ring; W is --(CH 2) 2 --, --CH CH-- or phenylene;X is a single bond, --CH CH--, --(CH 2) n --, or --O--(CH 2) n --; or X is branched alkylene or --O--branched alkylene wherein W is linked to Y through a chain n carbon atoms long;Y is --CO 2 H, --CO 2 alkyl, --CO 2 alkali metal, --CH 2 OH, --CONHSO 2 R 5, --CONHR 6, or --CH 2 -5-tetrazolyl;Z is O or NH;R 3 and R 4 are each independently hydrogen or alkyl or R 3 and R 4 together complete a ring optionally substituted through a ring carbon with a halo, lower alkyl, phenyl, halo (lower alkyl), halophenyl, oxo or hydroxyl group; and the remaining symbols are as defined in the specification.
