200572-33-4Relevant articles and documents
Regio- and Stereoselective Palladium-Catalyzed C(sp3)-H Arylation of Pyrrolidines and Piperidines with C(3) Directing Groups
Antermite, Daniele,Affron, Dominic P.,Bull, James A.
, p. 3948 - 3952 (2018/07/22)
The selective synthesis of cis-3,4-disubstituted pyrrolidines and piperidines is achieved by a Pd-catalyzed C-H arylation with excellent regio- and stereoselectivity using an aminoquinoline auxiliary at C(3). The arylation conditions are silver free, use a low catalyst loading, and employ inexpensive K2CO3 as a base. Directing group removal is accomplished under new, mild conditions to access amide-, acid-, ester-, and alcohol-containing fragments and building blocks. This C-H arylation protocol enabled a short and stereocontrolled formal synthesis of (-)-paroxetine.
CCR2 MODULATORS
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Paragraph 0187, (2016/12/07)
Compounds are provided that are modulators of the CCR2 receptor. The compounds have the general formula (I) and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activtation of CCR2 receptors.
PAROXETINE DERIVATIVE
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Paragraph 0113; 0114; 0115, (2013/08/14)
A compound represented by Formula (1), or a pharmacologically acceptable salt thereof retains the principal therapeutic effect of paroxetine and has an improved CYP inhibitory effect: wherein R1 is a hydrogen atom or C1-6 alkyl group