42331-02-2

Upstream product

• 3334-89-2 1-Phenylazetidine 
• 62-53-3 aniline 
• 109-64-8 1,3-dibromo-propane 
• 5003-71-4 3-bromopropylamine hydrochloride 
• 98-80-6 phenylboronic acid 

Downstream Products

• 3334-89-2 1-Phenylazetidine 
• 753491-51-9 4-[3-(3-bromo-propyl)-3-phenyl-ureido]-benzoic acid ethyl ester 
• 100303-11-5 N-[3-(methylphenethylamino)propyl]-N-phenylpropionamide 
• 1235866-13-3 9-O-[3-(phenylamino)propyl]berberine bromide 
• 1001197-97-2 1-phenyl-1,2,3,4-tetrahydrobenzo[h]quinoline 
• 1001197-96-1 8-methyl-1-phenyl-1,2,3,4-tetrahydroquinoline 
• 753491-59-7 4-(2-oxo-3-phenyl-tetrahydro-pyrimidin-1-yl)-benzoic acid ethyl ester 

Relevant academic research and scientific papers

Fe(III)-Catalyzed Aerobic Intramolecular N-N Coupling of Aliphatic Azides with Amines

An Fe(III)-catalyzed intramolecular N-N coupling of aliphatic azidoamines that forms diverse five- and six-membered semisaturated diazoheterocycles using air as an oxidant is reported, providing an alternative to hydrazine-based methods. Mechanistic studies suggest that a N-radical induced intramolecular homolytic substitution (SH2) is involved in ring closure. The power of this N-N bond-forming method is also demonstrated by using it as the final step in a total synthesis of (-)-newbouldine.

Fentanyl family at the mu-opioid receptor: Uniform assessment of binding and computational analysis

Interactions of 21 fentanyl derivatives with μ-opioid receptor (μOR) were studied using experimental and theoretical methods. Their binding to μOR was assessed with radioligand competitive binding assay. A uniform set of binding affinity data contains val

Site-Selective Conversion of Azido Groups at Carbonyl α-Positions to Diazo Groups in Diazido and Triazido Compounds

This paper reports on the selective conversion of alkyl azido groups at the carbonyl α-position to diazo compounds. Through β-elimination of dinitrogen, followed by hydrazone formation/decomposition, α-azidocarbonyl moieties were transformed into α-diazo carbonyl groups in one step. As these reaction conditions do not involve aryl or general alkyl azides, site-selective conversions of di- and triazides were achieved. Through this method, the successive site-selective conjugation of the triazido molecule with three different components is demonstrated.

Synthesis and biological evaluation of a new series of berberine derivatives as dual inhibitors of acetylcholinesterase and butyrylcholinesterase

A series of novel berberine derivatives were designed, synthesized, and biologically evaluated as inhibitors of both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Among these derivatives, compound 48a, berberine linked with 3-methylpyridi

Synthesis of benzannulated N-heterocycles by a palladium-catalyzed C-C/C-N coupling of bromoalkylamines

(Chemical Equation Presented) A palladium-catalyzed domino intermolecular alkylation/intramolecular amination of functionalized aryl iodides represents a new strategy for the synthesis of benzannulated N-heterocycles, affording functionalized indolines an

Design and synthesis of cyclic urea compounds: A pharmacological study for retinoidal activity

Retinoids are natural and synthetic analogues of all-trans retinoic acid (ATRA). Cancer and other serious hyperproliferative diseases are attractive therapeutic targets for retinoids. We report here the design and synthesis of novel cyclic urea compounds with retinoidal activity. YR105 exhibited potent differentiation-inducing ability toward human promyelocytic leukemia HL-60 cells at the concentration of 10-9M: its potency was almost equal to that of the native ligand, all-trans retinoic acid.

Ligand- and Base-Free Copper(II)-Catalyzed C-N Bond Formation: Cross-Coupling Reactions of Organoboron Compounds with Aliphatic Amines and Anilines

(Equation presented) A ligandless and base-free Cu-catalyzed protocol for the cross-coupling of arylboronic acids and potassium aryltrifluoroborate salts with primary and secondary aliphatic amines and anilines is described. The process utilizes catalytic copper(II) acetate monohydrate and 4 A molecular sieves in dichloromethane at slightly elevated temperatures under an atmosphere of oxygen. A broad range of functional groups are tolerated on both of the cross-coupling partners.

Imidazolyl derivatives as corticotropin releasing factor inhibitors

The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF receptor”) useful for the treatment of depression, anxiety, affective disorders, feeding disorders, post-traumatic stress disorder, headache, drug addiction, inflammatory disorders, drug or alcohol withdrawal symptoms and other conditions the treatment of which can be effected by the antagonism of the CRF-1 receptor.

Ring-opening Reactions. Stability and Reactivity of Aziridinium and Azetidinium Ions in Solution

Measurement of the equilibrium constant for the formation of 1-phenylazetidinium ion in solution together with an estimate of the upper limit of the corresponding quantity for 1-phenylaziridinium, reveals an unexpected difference of at least 1E9 in favour of the 4-membered ring.