188869-24-1Relevant articles and documents
Procee for the racemisation of 1-benzyl-4-(4-fluorophenyl)-3-hydroxymethyl-1,2-3,6-tetrahydropyridine to be used as intermediate in the synthesis of paroxetine
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, (2008/06/13)
A process for the racemisation of enantiomerically enriched 1-benzyl-4-(4-fluorophenyl)-3-hydroxymethyl-1,2,3,6-tetrahydropyridine which is a useful intermediate in the preparation of paroxetine. Formula (A) means that the compound (I) has an enantiomeric excess of one enantiomer over the other enantiomer. R1 and R2 are defined as in claim 1.
A convenient synthesis of (-)-paroxetine
Czibula, Laszlo,Nemes, Andras,Seboek, Ferenc,Szantay Jr., Csaba,Mak, Marianna
, p. 3336 - 3339 (2007/10/03)
A convenient synthesis of the antidepressant paroxetine starting from 1-benzyl-4-piperidone (2) is reported. A stereoselective reduction resulted in cis-piperidine-3-methanol [(+)-6]. The reaction between cis-piperidine-3- methanol mesylate (7) and sesamol led to benzyl-protected trans-paroxetine (9) through an inversion reaction of the stereogenic center at position 3. The latter compound was deprotected by hydrogenolysis. Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2004.
Piperidine derivatives having renin inhibiting activity
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, (2008/06/13)
Novel piperidine derivatives, their manufacture and use as medicaments, are disclosed. The invention is concerned with the novel piperidine derivatives of general formula I wherein R1, R2, R3, R4, Q, X, Z, m and n are as described herein.