- Polycyclic Azetidines and Pyrrolidines via Palladium-Catalyzed Intramolecular Amination of Unactivated C(sp3)-H Bonds
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A novel strategy to construct complex polycyclic nitrogen-containing heterocycles from aliphatic amines via picolinamide-assisted palladium-catalyzed C-H bond activation reaction was reported. The reaction exhibits broad substrate scope for the synthesis of various azabicyclic scaffolds, including azetidines and tropane-class alkaloids. Application of this method to naturally occurring (-)-cis-myrtanylamine, an unprecedented type of carbon-carbon bond activation, in which the electron-pair involved initiates an intramolecular "SN2-like" displacement of a cyclopalladium-fragment from a tertiary center, is described.
- Zhao, Jie,Zhao, Xiao-Jing,Cao, Pei,Liu, Ji-Kai,Wu, Bin
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- A class of nitrogen-containing heterocyclic butane framework of non-natural amino acid derivative and its synthesis method (by machine translation)
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The invention belongs to the technical field of chemical synthesis, in particular discloses a containing azetidine skeleton of the synthesis method of the non-natural amino acid derivatives, its target product non-natural amino acid derivatives of the formula such as the specification of the Chinese (I), (II), (III), (IV) and (V) as shown in the, in the formula compound is a nitrogen-containing heterocyclic butane framework of non-naturalα-,β- Andγ- Amino acid derivatives, nitrogen atom are 2 - pyridine carboxylic acid protection; carboxyl methyl esterification; formula (I) in order to contain the azetidine framework of non-naturalα- Amino acid derivatives; (II) for the formula containing azetidine bridge ring skeleton of non-naturalα- Amino acid derivatives, wherein n=1 or 2; type (III) is a nitrogen-containing heterocyclic butane and ring skeleton of non-naturalα- Amino acid derivatives; formula (IV) is a nitrogen-containing heterocyclic butane bridge ring skeleton of non-naturalβ- Amino acid derivatives; type (V) is a nitrogen-containing heterocyclic butane and ring skeleton of non-naturalγ- Amino acid derivatives. The experiment of this invention result proves that: the compounds have potential hypolipidemic activity. (by machine translation)
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- INHIBITORS OF HEPATITIS C VIRUS NS3/NS4A SERINE PROTEASE
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The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as me
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Page/Page column 76-77
(2008/06/13)
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