- Catalytic Asymmetric Synthesis of Cyclohexanes by Hydrogen Borrowing Annulations
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Hydrogen borrowing catalysis serves as a powerful alternative to enolate alkylation, enabling the direct coupling of ketones with unactivated alcohols. However, to date, methods that enable control over the absolute stereochemical outcome of such a process have remained elusive. Here we report a catalytic asymmetric method for the synthesis of enantioenriched cyclohexanes from 1,5-diols via hydrogen borrowing catalysis. This reaction is mediated by the addition of a chiral iridium(I) complex, which is able to impart high levels of enantioselectivity upon the process. A series of enantioenriched cyclohexanes have been prepared and the mode of enantioinduction has been probed by a combination of experimental and DFT studies.
- Armstrong, Roly J.,Akhtar, Wasim M.,Young, Tom A.,Duarte, Fernanda,Donohoe, Timothy J.
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supporting information
p. 12558 - 12562
(2019/08/16)
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- Radical C(sp2)-H Trifluoromethylation of Aldehydes in Aqueous Solution
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The copper-mediated C(sp2)-H trifluoromethylation of aldehydes is described. The reaction of aldehydes with (bpy)Cu(CF3)3, Et3SiH, and K2S2O8 in aqueous acetone at room temperatu
- Zhang, Pei,Shen, Haigen,Zhu, Lin,Cao, Weiguo,Li, Chaozhong
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supporting information
p. 7062 - 7065
(2018/11/21)
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- NOVEL 4-(2FUROYL)AMINOPIPERIDINES, INTERMEDIATES IN SYNTHESIZING THE SAME,PROCESS FOR PRODUCING THE SAME AND MEDICINAL USE OF THE SAME
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There are provided novel 4-(2-furoyl)aminopiperidines represented by the general formula (I), their synthetic intermediates, processes for their preparation and medicaments containing them. In the above formula, X is CH or N, and Y is a group of the following general formula (II), formula (II-a) or formula (III): wherein a, b and c are each an integer of 0-6; Z is CH2 or NH; W is O or S; T is O or N-R15 wherein R15 is H, a C1-C6 alkyl group, a benzyl group or a phenethyl group; and R1 is H, a C1-C6 alkoxycarbonyl group, a benzyloxycarbonyl group, or the like.The 4-(2-furoyl) aminopiperidine derivatives according to this invention possess opioid μ antagonistic activity and are useful for the treatment or prevention of side effects which are caused by μ receptors agonist and which are selected from constipation, nausea/emesis or itch, or for the treatment or prevention of idiopathic constipation, postoperative ileus, paralytic ileus, irritable bowel syndrome or chronic pruritus.
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