87289-73-4Relevant articles and documents
A 4-substituted piperidine derivatives synthetic method
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Paragraph 0135-0141, (2020/02/07)
The invention relates to a synthesis method of 4-substituted piperidine derivatives. The synthesis method comprises the following steps: continuously reacting alpha-single substituted acetonitrile serving as a raw material with two-molecular ethylene oxide in the presence of a base I, thereby synthesizing compounds (2), wherein not one compound (2) is generated, and the compounds (2) are in tautomeric equilibrium with a compound (6); breaking the balance in the presence of a base II to generate an alcoxyl negative ion compound (3); reacting the compound (3) with R2SO2X or (R2SO2)2O to generate sulphonates (4); performing a cyclization reaction on the sulphonates (4) and primary amine to synthesize 4-substituted piperidine derivatives. Compared with a document reported method, the synthesis method has the advantages that the reaction steps are shortened and the synthetic efficiency is improved.
COMPOUNDS AND COMPOSITIONS USEFUL AS CATHEPSIN S INHIBITORS
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Page/Page column 47, (2008/06/13)
The present invention relates to the use of a 2-cyanopyrimidine compound of the formula (I), wherein R1, R2, R3 and X are as defined in the specification and in the claims, in free form or in salt form, and , where possible, in tautomeric form, as an inhibitor of the activity of cathepsin S.
Facile Synthesis of N-Substituted-4-cyano-4-phenylpiperidines via Phase-Transfer Catalysis
Thompson, Doug,Reeves, Perry C.
, p. 771 - 772 (2007/10/02)
Phenylacetonitrile can be condensed with N-substituted-bis(2-chloroethyl)amines in aqueous sodium hydroxide solution to produce N-substituted-4-cyano-4-phenylpiperidines.Hexadecyltributylphosphonium bromide is an effective catalyst for this phase-transfer reaction.
