14176-52-4Relevant articles and documents
Structure-activity relationships for the anaesthetic and analgaesic properties of aromatic ring-substituted ketamine esters
Bickerdike, Michael J.,Denny, William A.,Dimitrov, Ivaylo V.,Harvey, Martyn G.,Sleigh, James W.,Voss, Logan J.
, (2020)
A series of benzene ring substituted ketamine N-alkyl esters were prepared from the corresponding substituted norketamines. Few of the latter have been reported since they have not been generally accessible via known routes. We report a new general route to many of these norketamines via the Neber (oxime to α-aminoketone) rearrangement of readily available substituted 2-phenycyclohexanones. We explored the use of the substituents Cl, Me, OMe, CF3, and OCF3, with a wide range of lipophilic and electronic properties, at all available benzene ring positions. The 2- and 3-substituted compounds were generally more active than 4-substituted compounds. The most generally acceptable substituent was Cl, while the powerful electron-withdrawing substituents CF3 and OCF3 provided fewer effective analogues.
Intermediate compound for synthesizing tiletamine and synthesis method of tiletamine
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Paragraph 0043; 0046; 0047; 0048, (2019/02/04)
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.
