72219-19-3

Upstream product

• 142335-64-6 4-(pyrrolidin-1-ylmethyl)aniline 
• 123-75-1 pyrrolidine 
• 123-11-5 4-methoxy-benzaldehyde 
• 123-08-0 4-hydroxy-benzaldehyde 
• 100-14-1 4-nitrobenzyl chloride 
• 133851-67-9 1-(4-nitro-benzyl)-pyrrolidine 

Downstream Products

• 1234202-15-3 4-(pyrrolidin-1-ylmethyl)phenyl-3-(1H-indol-3-yl)propanoate 
• 1234202-13-1 4-(pyrrolidin-1-ylmethyl)phenyl-2-(1H-indol-3-yl)acetate 
• 1354792-29-2 tert-butyl 3-(4-(pyrrolidin-1-ylmethyl)phenoxy)azetidine-1-carboxylate 
• 1354791-20-0 (5-(4-chlorophenyl)-1,3,4-oxadiazol-2-yl)(3-(4-(pyrrolidin-1-ylmethyl)phenoxy)azetidin-1-yl)methanone 
• 1354792-30-5 1-(4-(azetidin-3-yloxy)benzyl)pyrrolidine 
• 1354791-23-3 (5-(4-fluorophenyl)-1,3,4-oxadiazol-2-yl)(3-(4-(pyrrolidin-1-ylmethyl)phenoxy)azetidin-1-yl)methanone 
• 1354791-22-2 (5-phenyl-1,3,4-oxadiazol-2-yl)(3-(4-(pyrrolidin-1-ylmethyl)phenoxy)azetidin-1-yl)methanone 
• 1354791-21-1 (5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)(3-(4-(pyrrolidin-1-ylmethyl)phenoxy)azetidin-1-yl)methanone 

Relevant academic research and scientific papers

Synthesis and biological evaluation of a new class of multi-target heterocycle piperazine derivatives as potential antipsychotics

In this study, we designed and synthesized a novel series of multi-receptor ligands as polypharmacological antipsychotic agents by using a multi-receptor affinity strategy. Among them,3wcombines a multi-receptor mechanism with high mixed affinities for D

NITROGEN-CONTAINING HETEROCYCLIC RING SUBSTITUTED DIHYDROARTEMISININ DERIVATIVES AND USE THEREOF

The present invention belongs to the field of medicinal technique, specifically relates to nitrogen-containing heterocyclic ring-substituted dihydroartemisinin derivatives and their optical isomers according to formula I or II; wherein substituent X, Y, r

Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties

A novel series of melanin concentrating hormone receptor 1 (MCHr1) antagonists were the starting point for a drug discovery program that culminated in the discovery of 103 (AZD1979). The lead optimization program was conducted with a focus on reducing lipophilicity and understanding the physicochemical properties governing CNS exposure and undesired off-target pharmacology such as hERG interactions. An integrated approach was taken where the key assay was ex vivo receptor occupancy in mice. The candidate compound 103 displayed appropriate lipophilicity for a CNS indication and showed excellent permeability with no efflux. Preclinical GLP toxicology and safety pharmacology studies were without major findings and 103 was taken into clinical trials.

HISTAMINE-3 RECEPTOR ANTAGONISTS

This invention is directed to a compound of the formula Ia or Ib. as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a method of treatment of a disorder or condition that may be treated by antagonizing histamine H3 receptors, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above, and a method of treatment of a disorder or condition selected from the group consisting of depression, mood disorders, schizophrenia, anxiety disorders, Alzheimer's disease, attention-deficit disorder (ADD), attention-deficit hyperactivity disorder (ADHD), psychotic disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy- induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the Gl tract, hyper and hypo motility and acidic secretion of the gastro- intestinal tract, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above.

Design, synthesis, and evaluation of 2-phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors

A series of 2-phenoxy-indan-1-one derivatives have been designed, synthesized, and tested as acetylcholinesterase inhibitors. The most potent compound exhibited high AChE inhibitory activity (IC50 = 50 nM), and the molecular docking study indicated that it was nicely accommodated by AChE.

Bicyclic compounds

Substituted N-substituted alkoxyphenyl compounds, compositions containing them, and methods of making and using them.

Efficient and chemoselective deoxygenation of amine N-oxides using polymethylhydrosiloxane

Deoxygenation of aromatic and aliphatic amine N-oxides to the corresponding amines is achieved under mild conditions. The reagent combination employed for this transformation is polymethylhydrosiloxane (PMHS) in the presence of either tetrakis (triphenylphosphine) palladium (0) [Pd(PPh3)4], titanium (IV) isopropoxide [Ti(i-PrO)4] or palladium on carbon (Pd/C).

Structure-activity studies on a 1,2,3-triazole derivative, a potent in vitro inhibitor of prostaglandin synthesis: The role of the heterocyclic ring

This paper reports further structural modifications concerning the 1,2,3- triazole ring of the compound A, an effective in vitro inhibitor of prostaglandin synthesis. The introduction of different heterocyclic rings provided further information about of t

Trapping of Metabolically Generated Electrophilic Species with Cyanide Ion: Metabolism of 1-Benzylpyrrolidine

Incubations of 1-benzylpyrrolidine (4) and specifically deuterium-labeled analogues of 4 with rabbit liver microsomal preparations in the presence of cyanide ion have led to the characterization of 1-benzyl-2-cyanopyrrolidine (13), cis- and trans-1-benzyl