167262-37-5

Upstream product

• 98-88-4 benzoyl chloride 
• 52423-89-9 3-(3,4-dichloro-phenyl)-3-(2-hydroxy-ethyl)-pyrrolidine 
• 193755-82-7 1-Benzoyl-3-(3,4-dichlorophenyl)-3-(2-[tetrahydropyran-2-yloxy]ethyl)pyrrolidine 
• 3218-49-3 3,4-dichloro-benzeneacetonitrile 
• 135936-16-2 α-[2-(Tetrahydropyran-2-yloxy)ethyl]-3,4-dichlorophenyl-acetonitrile 
• 155308-39-7 4-(3,4-dichloro-phenyl)-4-[2-(tetrahydro-pyran-2-yloxy)-ethyl]-pyrrolidine 
• 155308-38-6 4-(3,4-dichloro-phenyl)-4-[2-(tetrahydro-pyran-2-yloxy)-ethyl]-pyrrolidin-2-one 
• 155308-37-5 3-cyano-3-(3,4-dichloro-phenyl)-5-(tetrahydro-pyran-2-yl-oxy)-pentanoic acid ethyl ester 
• 40878-10-2 3-cyano-3-(3,4-dichloro-phenyl)-pentanedioic acid diethyl ester 
• 40878-11-3 [3-(3,4-dichloro-phenyl)-5-oxo-pyrrolidin-3-yl]-acetic acid ethyl ester 

Downstream Products

• 167262-38-6 2-[1-Benzoyl-3-(3,4-dichloro-phenyl)-pyrrolidin-3-yl]-ethyl methanesulfonate 
• 193755-84-9 1-Benzoyl-3-(3,4-dichlorophenyl)-3-(formylmethyl)pyrrolidine 

Relevant academic research and scientific papers

4-Amino-2-(aryl)-butylbenzamides and their conformationally constrained analogues. Potent antagonists of the human neurokinin-2 (NK2) receptor

A library, evaluating a range of piperazines, piperidines and acyclic amines, as replacements for the 4-hydroxy-4-phenylpiperidine moiety in lead (1b) was prepared. These efforts identified the 4-((N)-benzimidazolone)piperidine analogue (2a) which was further optimised using classical single-compound synthesis to yield the 3-((N)-morpholino)azetidine (2j). Conformationally constrained analogues of (2j), generally offered no potency advantage in this particular series.

3-Azetidinylalkylpiperidines or -pyrrolidines as tachykinin antagonists

The present invention provides compounds of formula (I) and the pharmaceutically acceptable salts thereof. Such compounds and salts are tachykinin antagonists.

SUBSTITUTED PYRROLIDIN-3-YL-ALKYL-PIPERIDINES

The present invention relates to substituted pyrrolidinyl-3-yl-alkyl-piperidines, their stereoisomers, and pharmaceutically acceptable salts thereof and processes for preparation of the same. The compounds of the present invention are useful in their pharmacological activities such as tachykinin antagonism, especially substance P and neurokinin A antagonism, and the like. Compounds having the property of tachykinin antagonism are indicated for conditions associated with neurogenic inflammation and other diseases described herein.

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