172734-70-2Relevant articles and documents
Construction of Quaternary Carbon Center by Catalytic Asymmetric Alkylation of 3-Arylpiperidin-2-ones Under Phase-Transfer Conditions
Inukai, Tomoaki,Kano, Taichi,Maruoka, Keiji
, p. 2211 - 2214 (2020/01/08)
A highly enantioselective synthesis of δ-lactams having a chiral quaternary carbon center at the α-position has been developed through an asymmetric alkylation of 3-arylpiperidin-2-ones under phase-transfer conditions. In this transformation, a 2,2-diarylvinyl group on the δ-lactam nitrogen atom plays a crucial role as a novel protecting group and an achiral auxiliary for improving both yield and enantioselectivity of the reaction.
3-Azetidinylalkylpiperidines or -pyrrolidines as tachykinin antagonists
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, (2008/06/13)
The present invention provides compounds of formula (I) and the pharmaceutically acceptable salts thereof. Such compounds and salts are tachykinin antagonists.
Azetidinylpropylpiperidine derivatives, intermediates and use as tachykinin antagonists
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, (2008/06/13)
Compounds of the formula (I): where X1, A, Ar1, X and R are as defined in the specification, and pharmaceutically-acceptable salts thereof, are new, and are useful as tachykinin inhibitors which act at the NK1, NK2and NK3receptors or a combination of two or more thereof.
A practical and scalable synthesis of SR 142801, a tachykinin NK3 antagonist
Chen, Huai G.,Chung,Goel,Johnson,Kesten,Knobelsdorf,Lee,Rubin
, p. 555 - 560 (2007/10/03)
A practical and scalable total synthesis of tachykinin NK3 receptor antagonist SR 142801, (R)-N-[1-[3-[1-benzoyl-3-(3,4-dichlorophenyl)-3-piperidinyl]propyl]-4-phenyl-4 -piperidinyl]-N-methyl acetamide 1 is described. The absolute configuration of the key intermediate 7 was determined by single crystal X-ray crystallography, on the basis of which, the absolute configuration of SR 142801 should be (R)-(+), instead of the recently reported (S)-(+).