61270-20-0

Upstream product

• 111-24-0 1,5-dibromo-pentane 
• 150-19-6 O-methylresorcine 
• 629-03-8 1 ,6-dibromohexane 
• 150-76-5 4-methoxy-phenol 

Downstream Products

• 1446339-32-7 (S)-3-{1-[5-(3-methoxyphenoxy)pentyl]piperidin-2-yl}pyridine oxalate 

Relevant academic research and scientific papers

Application of propynylamine derivative in pharmacy

The invention discloses application of a propynylamine derivative in pharmacy. Shown by tests of the applicant, the derivative can selectively inhibit MAO-B, is remarkable in activity and can be usedfor preparing MAO-B inhibitors and drugs for preventing

Propargylamine derivative and synthesis method thereof

The invention discloses a series of propargylamine derivatives and a synthesis method thereof. The synthesis method of the derivative mainly comprises the following steps: (1) putting any one of the structures shown in the following formulas (A)-(E) and e

Design, synthesis and biological evaluation of rasagiline-clorgyline hybrids as novel dual inhibitors of monoamine oxidase-B and amyloid-β aggregation against Alzheimer's disease

A series of rasagiline-clorgyline hybrids was designed, synthesized and investigated in vitro for their inhibition of monoamine oxidase and amyloid-β aggregation. Most of compounds were found to be selective and highly potent hMAO-B inhibitors showing IC50 values in the nanomolar, and exhibited a moderate inhibition of amyloid-β aggregation. 7-((5-(methyl(prop-2-yn-1-yl)amino) pentyl)oxy)chroman-4-one (6j) was the most interesting compound identified in this research, endowed with higher hMAO-B potency (IC50 = 4 nM) and selectivity (SI > 25000) compared to the reference selective inhibitor rasagiline (IC50 = 141 nM, SI > 355), and exhibited good inhibitory activity against Aβ1-42 aggregation (40.78percent, 25 μM). Kinetic and molecular modeling studies revealed that 6j was a competitive reversible inhibitor for hMAO-B. Moreover, compound 6j displayed low toxicity and good neuroprotective effects in SH-SY5Y cell assay, and could penetrate the blood-brain barrier according to the parallel artificial membrane permeability assay. Pharmacokinetics assay revealed that compound 6j possessed good pharmacokinetic profiles after intravenous and oral administrations. Overall, these results highlighted that compound 6j was an effective and promising multitarget agent against Alzheimer's disease.

Synthesis of N-aryloxyalkylanabasine derivatives

N-Aryloxyalkylanabasine derivatives were prepared via the reaction of anabasine hydrochloride with various aryloxyhaloalkanes in the presence of potash in DMF. The reaction occurred with retention of the chiral center C-(2) of the piperidine group. Side products of bis(aryloxy)ethanes were characterized.