Transition-metal-free α-arylation of nitroketones with diaryliodonium salts for the synthesis of tertiary α-aryl, α-nitro ketones
Transition-metal-free α-arylation of α-nitroketones with diaryliodonium salts has been realized for the first time. As an application of this methodology, a concise synthesis of the clinical drug tiletamine was also achieved via a three-step procedure from 2-nitrocyclohexanone without the isolation of intermediates.
An, Yang,Zhang, Xiao-Ming,Li, Ze-Yu,Xiong, Wen-Hui,Yu, Run-Dong,Zhang, Fu-Min
p. 119 - 122
(2019/01/03)
Intermediate compound for synthesizing tiletamine and synthesis method of tiletamine
The invention discloses an intermediate compound for synthesizing tiletamine. The intermediate compound adopts a chemical structural formula as shown in the description. The intermediate compound is obtained by performing a reaction on bis(2-thienyl)iodate and 2-nitrocyclohexanone under the action of alkali, and with the intermediate compound as a substrate, the tiletamine is produced through nitroreduction and aminoethylation. Compared with the existing synthesis method of the tiletamine, the synthesis method of the tiletamine, provided by the invention, has the advantages of a simple route,low cost and convenience in operation.
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(2019/02/04)
Sequential [3,3]-Sigmatropic Rearrangement/Nucleophilic Arylation of N -(Benzoyloxy)enamides towards the Preparation of Cyclic β-Aryl-β-amino Alcohols
A new method has been developed for the efficient synthesis of cyclic β-aryl-β-amino alcohol derivatives bearing a tetrasubstituted carbon center via the [3,3]-sigmatropic rearrangement of N-(benzoyl oxy)enamides followed by nucleophilic arylation reactio