69311-30-4

Upstream product

• 628-20-6 4-Chlorobutyronitrile 
• 6921-34-2 benzylmagnesium chloride 
• 1589-82-8 phenylmagnesium bromide 
• 5332-06-9 4-bromobutanenitrile 
• 127808-49-5 5-phenylpent-4-yn-1-amine 
• 101-97-3 Ethyl 2-phenylethanoate 
• 536-74-3 phenylacetylene 
• 24463-87-4 (5-chloropent-1-ynyl)benzene 
• 152711-26-7 3-phenylacetyl-1-vinyl-pyrrolidin-2-one 

Downstream Products

• 35840-91-6 2-benzylpyrrolidine 
• 116993-29-4 6-n-butyl-7-hydroxy-8-phenyl-2,3-dihydro-1H-indolizin-5-one 
• 104765-64-2 6-(4-chlorophenyl)-7-phenyl-2,3-dihydro-1H-pyrrolizin 
• 823821-72-3 N-(4-oxo-5-phenylpentyl)acetamide 
• 882696-35-7 2-benzyl-1-(phenylsilyl)pyrrolidine 
• 156897-17-5 <6-(4-chlorophenyl)-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl>-acetic acid 
• 156897-46-0 <6-(4-chlorophenyl)-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl>-acetic acid-ethylester 
• 1027239-58-2 2-(4-methylsulfinyl-phenyl)-1-phenyl-6,7-dihydro-5H-pyrrolizine 
• 1204423-05-1 3-(3-phenyl-1H-indol-2-yl)propylamine hydrochloride 

Relevant academic research and scientific papers

Cyclooxygenase-1/2 (COX-1/COX-2) and 5-lipoxygenase (5-LOX) inhibitors of the 6,7-diaryl-2,3-1H-dihydropyrrolizine type

A series of 6,7-diaryl-2,3-1H-dihydropyrrolizines was prepared as COX-1/COX-2 and 5-LOX inhibitors. The inhibition of COX-1 was evaluated using intact bovine platelets as the enzyme source, whereas LPS-stimulated human monocytes served as the enzyme source for inducible COX-2. The determination of arachidonic metabolites was performed by HPLC for COX-1 and RIA for COX-2. The balance between COX-1/COX-2 and 5-LOX inhibition can be shifted by modifying the substitution pattern of the phenyl moiety at the 6- and 7-position of the pyrrolizine nucleus. Structure-activity relationships are discussed.

A Commercially Available and User-Friendly Catalyst for Hydroamination Reactions under Technical Conditions

The activity of a simple, commercially available copper salt, [Cu(NCMe)4](BF4) in intramolecular hydroamination reactions of alkynes and allenes is presented. Reactions were successfully carried out in technical acetonitrile in the presence of air. While attempts of alkene hydroamination failed, this catalyst was also found active in intermolecular aza-Michael reactions.

Zinc-zinc bonded decamethyldizincocene Zn2(η5- C5Me5)2 as catalyst for the inter- and intramolecular hydroamination reaction

The Zn-Zn bonded compound [(η5-Cp*)2Zn 2] was investigated as catalyst for the inter- and intramolecular hydroamination reaction. High reaction rates under mild conditions were observed. This is the first application of a

2-(CYCLIC AMINO)-PYRIMIDONE DERIVATIVES AS TPK1 INHIBITORS

A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof (I) wherein R2 represents a hydrogen or the like; R3 represents methyl group or the like; R20 represents a halogen atom or the like; q represents an integer of 0 to 3; Z represent nitrogen atom, CH, or the like; R4 represents hydrogen or the like; R5 represents hydrogen or the like; R6 represents a substituted alkyloxy and the like; p represents an integer of 0 to 3; X represents bond, CH2, oxygen atom, NH, or the like; any one or more of R5 and R6, R5 and R4, R6 and R4, X and R5, X and R4, X and R6, and R6 and R6 may combine to each other to form a ring, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).

Convenient synthesis of melatonin analogues: 2- and 3-substituted -N-acetylindolylalkylamines

A new method for the synthesis of 2- and 3-substituted indolylalkylamides, derivatives of melatonin, from arylhydrazines and amidoketones by the Fischer reaction was elaborated. The amidoketones can be easily prepared from cyclic imines by reaction with acylpyridinium chloride. This method is a one-step synchronous creation of the selected alkylamide fragment and the indole core. Variation of the arylhydrazines create the desired substituents in the carbocycle of indolylalkylamides and suitable choice of amidoketone can direct the amidoalkyl chain to the 2- or 3-position of the indole. Graphical Abstract

FUSED PYRROLE COMPOUNDS, PHARMACEUTICAL AGENTS CONTAINING THE SAME, AND THE USE THEREOF

The present invention relates to fused pyrrole compounds of the formula 1. in which at least one of the radicals R1, R2, R3 is 4-sulphur-substituted phenyl. These compounds are in particular pyrrolizines, indolizines and heteroanalogues having selective inhibitory action on isoenzyme-2 of prostaglandin H synthase (COX-2). The invention also relates to pharmaceutical compositions which contain these compounds; and the use of these compounds for the treatment of disorders of the rheumatic type.

A PRACTICAL PREPARATION OF Δ1-2-SUBSTITUTED AND Δ1-2,3-DISUBSTITUTED PYRROLINES

Addition of N-vinylpyrrolidinone and an ester to NaH in THF effects acylation and affords keto lactams (1) in high yields.Hydrolysis of 1 in strong acid generates Δ1-2-substituted pyrrolines (2) in good yield.Keto lactams (1) can be further alkylated and hydrolyzed to produce Δ1-2,3-disubstituted pyrrolines (4) in good isolated yield.

THE PREPARATION OF "ELONGATED" NICOTINE ANALOGUES

The preparation of four nicotine analogues having one or two additional methylene units between the N-methylpyrrolidinyl moiety and the aromatic ring are reported.Also prepared are the corresponding nornicotine and myosmine analogues.The course of the Spa