40981-73-5

Upstream product

• 103-90-2 4-acetaminophenol 
• 109-64-8 1,3-dibromo-propane 
• 2623-33-8 4-acetoxyacetanilide 
• 123-30-8 4-amino-phenol 

Downstream Products

• 85868-56-0 1-(4-acetamidophenoxy)-3-1-(N⁴-(3-trifluoromethylphenyl)piperazinyl)>propane 
• 85868-53-7 1-(4-acetamidophenoxy)-3-1-(N⁴-(2-methoxyphenyl)piperazinyl)>propane 
• 1374606-82-2 N-(4-(3-bromopropoxy)-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)acetamide 
• 1119120-33-0 N-[4-(3-nitrooxy-propoxy)-phenyl]-acetamide 

Relevant academic research and scientific papers

Transition metal- And light-free radical borylation of alkyl bromides and iodides using silane

We report operationally simple and neutral conditions for borylation of alkyl bromides and iodides to alkyl boronic esters under transition metal- and light-free conditions. A series of substrates with a wide range of functional groups were effectively transformed into the borylation products in moderate to good yields. Mechanistic studies, including radical clock experiments and DFT calculations, gave detailed insight into the radical borylation process.

Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics

We report the optimisation of a series of novel amide-piperidine (piperazine) derivatives using the multiple ligand approach with dopamine and serotonin receptors. Of the derivatives, compound 11 exhibited high affinity for the D2, 5-HT1A, and 5-HT2A receptors, but low affinity for the 5-HT2C and histamine H1 receptors and human ether-a-go-go-related gene (hERG) channels. In vivo, compound 11 reduced apomorphine-induced climbing, MK-801-induced hyperactivity and DOI-induced head twitching without observable catalepsy, even at the highest dose tested. In addition, it exhibited suppression in a CAR test. Furthermore, in a novel object recognition task, it displayed procognition properties. Therefore, compound 11 is a promising candidate multi-target antipsychotic.

Transition-Metal-Free Borylation of Alkyl Iodides via a Radical Mechanism

We describe an operationally simple transition-metal-free borylation of alkyl iodides. This method uses commercially available diboron reagents as the boron source and exhibits excellent functional group compatibility. Furthermore, a diverse range of prim

NITRIC OXIDE RELEASING DERIVATIVES OF PARACETAMOL

The present invention particularly relates to novel nitrate esters of paracetamol. The nitrate esters of paracetamol are prepared by reacting the paracetamol with dihaloalkyl compound and followed by reaction with silver nitrate to obtain the correspondin

NITRIC OXIDE RELEASING DERIVATIVES OF PARACETAMOL

The present invention particularly relates to novel nitrate esters of paracetamol. The nitrate esters of paracetamol are prepared by reacting the paracetamol with dihaloalkyl compound and followed by reaction with silver nitrate to obtain the correspondin

Synthesis and Pharmacological Evaluation of 1-Oxo-2-(3-piperidyl)-1,2,3,4-tetrahydroisoquinolines and Related Analogues as a New Class of Specific Bradycardic Agents Possessing If Channel Inhibitory Activity

A series of 1-oxo-2-(3-piperidyl)-1,2,3,4-tetrahydroisoquinolines and related analogues were prepared and evaluated for their bradycardic activities in isolated right atrium and in anesthetized rats. (± )-6,7-Dimethoxy-2-{1- [3-(3,4-methylenedioxyphenoxy)propyl]-3-piperidyl}-1,2,3, 4-tetrahydroisoquinoline (4) was chosen as a lead, and structural modifications were performed on the tetrahydroisoquinoline ring and the terminal aromatic ring. The modifications on the tetrahydroisoquinoline ring revealed that the 1-oxo-1,2,3,4-tetrahydroisoquinoline ring system was optimum structure for both in vitro potency and in vivo efficacy. Furthermore, methoxy, ethoxy, and methoxycarbonyl groups were identified as preferable substituents on the terminal aromatic ring. One of the 1-oxo-1,2,3,4-tetrahydroisoquinoline derivatives, (R)-10a, was further evaluated for its bradycardic activity and inhibitory activity against If currents. Compound (R)-10a demonstrated potent bradycardic activity in rats with minimal influence on blood pressure after oral administration. The compound also showed inhibition of If currents (IC50 = 0.32 μM) in guinea pig pacemaker cells.