172734-92-8Relevant articles and documents
Crystalline forms of osanetant
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Page 4, (2010/02/05)
The invention relates to crystalline forms of (R)-(+)-N-[[3-[1-benzoyl-3-(3,4-dichlorophenyl)piperidin-3-yl]prop-1-yl]-4-phenylpiperidin-4-yl]-N-methylacetamide and to processes for preparing them.
COMPOUNDS WHICH ARE SELECTIVE ANTAGONISTS OF THE HUMAN NK3 RECEPTOR AND THEIR USE AS MEDICINAL PRODUCTS AND DIAGNOSTIC TOOLS
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, (2008/06/13)
A compound of formula: STR1 in which: Ar represents a pyrid-2-yl or a phenyl which is unsubstituted or substituted by a halogen, a methyl or a (C 1-C 4)alkoxy;R 1 represents a methyl group;R 11 represents hydrogen; or R 1 and R 11 toge
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)-(+).
A reliable and efficient synthesis of SR 142801
Giardina,Grugni, Mario,Rigolio, Roberto,Vassallo, Marco,Erhard, Karl,Farina, Carlo
, p. 2307 - 2310 (2007/10/03)
A convenient synthesis of the potent human NK-3 receptor antagonist SR 142801, (S)-(+)-N-{{3-[1-benzoyl-3-(3,4-dichlorophenyl)piperidin-3-yl]prop-1 -yl}-4-phenylpiperidin-4-yl}-N-methylacetamide [(S)-(+)-(15)], is described. Improvements over the previously reported procedure are the preparation of the intermediate 5 via the novel imide 3 and subsequent reaction with the nucleophile 14, which reacts, regioselectively, at the endocyclic nitrogen.