167263-23-2

Upstream product

• 52423-89-9 3-(3,4-dichloro-phenyl)-3-(2-hydroxy-ethyl)-pyrrolidine 
• 167263-94-7 3-Isopropoxy-phenyl-acetyl chloride 
• 3218-49-3 3,4-dichloro-benzeneacetonitrile 
• 40878-11-3 [3-(3,4-dichloro-phenyl)-5-oxo-pyrrolidin-3-yl]-acetic acid ethyl ester 
• 40878-10-2 3-cyano-3-(3,4-dichloro-phenyl)-pentanedioic acid diethyl ester 

Downstream Products

• 167263-24-3 3-(2-Methanesulfonyloxyethyl)-3-(3,4-dichlorophenyl)-1-(3-isopropoxyphenyl)acetylpyrrolidine 

Relevant academic research and scientific papers

1-AZONIABICYCLO[2.2.1]HEPTANES, METHODS OF PREPARING THEM AND PHARMACEUTICAL COMPOSITIONS IN WHICH THEY ARE PRESENT

The invention relates to quaternary basic amides of the formula STR1 in which Ar is an optionally substituted mono-, di-or tricyclic aromatic or heteroaromatic group;T is a direct bond, a hydroxymethylene group, an alkoxymethylene group in which the alkoxy group is C 1-C. sub.4, or a C 1-C 5-alkylene group; Ar' is an unsubstituted or mono-or poly-substituted phenyl, a thienyl, a benzothienyl, a naphthyl or an indolyl; R is hydrogen or a C 1-C. sub.4-alkyl, or a C 1-C 4-ω-alkoxy(C 2-C 4) alkyl, or a C 2-C 4-ω-alkanoyloxy (C 1-C 4)alkyl;.Q is hydrogen;or else Q and R together form a 1,2-ethylene, 1,3-propylene or 1,4-butylene group;Am ⊕ is the radical STR2 in which X 1, X 2 and X 3, together with the nitrogen atom to which they are bonded, form a 1-AZONIABICYCLO[2.2.1] HEPTANE optionally substituted by a phenyl or benzyl group; and A . crclbar. is a pharmaceutically acceptable anion. These compounds are useful for the preparation of drugs intended for the treatment of pathological conditions involving the tachykinin system.

1-AZONIABICYCLO[2.2.1] HEPTANES AND PHARMACEUTICAL COMPOSITIONS IN WHICH THEY ARE PRESENT

The invention relates to quaternary basic amides of the formula STR1 in which Ar is an optionally substituted mono-, di-or tri-cyclic aromatic or heteroaromatic group;T is a direct bond, a hydroxymethylene group, an alkoxymethylene group in which the alkoxy group is C 1-C. sub.4, or a C 1-C 5-alkylene group; Ar' is an unsubstituted or mono-or poly-substituted phenyl, a thienyl, a benzothienyl, a naphthyl or an indolyl; R is hydrogen or a C 1-C 4-alkyl, or a ω-C 1-C. sub.4-alkoxy(C 2-C 4) alkyl, or a ω-C 2-C. sub.4-alkanoyloxy (C 1-C 4)alkyl;.Q is hydrogen;or else Q and R together form a 1,2-ethylene, 1,3-propylene or 1,4-butylene group;Am ⊕ is the radical STR2 in which X 1, X 2 and X 3, together with the nitrogen atom to which they are bonded, form an azabicyclic or azatricyclic system optionally substituted by a phenyl or benzyl group; andA ? is a pharmaceutically acceptable anion.These compounds are useful for the preparation of drugs intended for the treatment of pathological conditions involving the tachykinin system.

Identification and chemical synthesis of MDL 105,212, a non-peptide tachykinin antagonist with high affinity for NK1 and NK2 receptors

We have synthesized and identified MDL 105,212, a non-peptide tachykinin receptor antagonist that has high affinity for human NK1 ((IC50 = 3.11 nM) and NK2 (IC50 = 8.40 nM) receptors. The chemical synthesis of M