23699-77-6

Upstream product

• 75-52-5 nitromethane 
• 24424-99-5 di-tert-butyl dicarbonate 
• 121-33-5 vanillin 
• 1477-68-5 3-Methoxytyramine hydrochloride 
• 554-52-9 3-Methoxytyramine 

Downstream Products

• 942301-95-3 [2-[4-(3-fluoro-benzyloxy)-3-methoxy-phenyl]-ethyl]-carbamic acid tert-butyl ester 
• 342880-36-8 tert-butyl 4-(cyanomethoxy)-3-methoxyphenethylcarbamate 
• 23428-81-1 3-Methoxy-4-benzyloxy-N-tert.-butyloxycarbonyl-phenaethylamin 
• 1860-57-7 [2-(4-benzyloxy-3-methoxyphenyl)ethyl]amine hydrochloride 
• 22231-61-4 2-[4-(benzyloxy)-3-methoxyphenyl]ethylamine 
• 19886-92-1 1-ethyl-7-hydroxy-6-methoxy-1,2,3,4-tetrahydroisoquinoline hydrochloride 
• 1032821-81-0 N-[2-(4-benzyloxy-3-methoxyphenyl)ethyl]propionamide 
• 51-61-6 dopamine 
• 37034-31-4 N-(tert-butoxycarbonyl)dopamine 

Relevant academic research and scientific papers

Synthesis and Evaluation of New Fluorine-18 Labeled Verapamil Analogs to Investigate the Function of P-Glycoprotein in the Blood-Brain Barrier

P-glycoprotein is an efflux transporter located in the blood-brain barrier. (R)-[11C]Verapamil is widely used as a PET tracer to investigate its function in patients with epilepsy, Alzheimer's disease, and other neurodegenerative diseases. Currently it is not possible to use this successful tracer in clinics without a cyclotron, because of the short half-life of carbon-11. We developed two new fluorine-18 labeled (R)-verapamil analogs, with the benefit of a longer half-life. The synthesis of (R)-N-[18F]fluoroethylverapamil ([18F]1) and (R)-O-[18F]fluoroethylnorverapamil ([18F]2) has been described. [18F]1 was obtained in reaction of (R)-norverapamil with the volatile [18F]fluoroethyltriflate acquired from bromoethyltosylate and a silver trilate column with a radiochemical yield of 2.7% ± 1.2%. [18F]2 was radiolabeled by direct fluorination of precursor 13 and required final Boc-deprotection with TFA resulting in a radiochemical yield of 17.2% ± 9.9%. Both tracers, [18F]1 and [18F]2, were administered to Wistar rats, and blood plasma and brain samples were analyzed for metabolic stability. Using [18F]1 and [18F]2, PET scans were performed in Wistar rats at baseline and after blocking with tariquidar, showing a 3.6- and 2.4-fold increase in brain uptake in the blocked rats, respectively. In addition, for both [18F]1 and [18F]2, PET scans in Mdr1a/b(-/-), Bcrp1(-/-), and WT mice were acquired, in which [18F]2 showed a more specific brain uptake in Mdr1a/b(-/-) mice and no increased signal in Bcrp1(-/-) mice. [18F]2 was selected as the best performing tracer and should be evaluated further in clinical studies.

1,4-DISUBSTITUTED PYRIDAZINE ANALOGS AND METHODS FOR TREATING SMN-DEFICIENCY-RELATED CONDITIONS

The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

1,2,3,4-TETRAHYDROISOQUINOLINE DERIVATIVES HAVING EFFECTS OF PREVENTING AND TREATING DEGENERATIVE AND INFLAMMATORY DISEASES

Provided are 7-hydroxy-6-methoxy-1,2,3,4-tetrahydroisoquinoline derivatives and synthesis methods thereof. The compounds significantly inhibit the production of nitrogen monoxide (NO) and superoxide in an activated microglial cell and expressions of TNF-α, IL-1β inducive NO synthase and cyclooxygenase-2 genes. They also prevent NF-kB shift to a nucleus, decrease reactive oxygen species (ROS), inhibit expression of GTP cyclohydrolase I gene and over-production of tetrahydrobiopterin (BH4), and protect dopaminergic neurons from injury due to activated microglial cells. Consequently, the compounds are effective in treating inflammatory and neurodegenerative diseases.

1,2,3,4-TETRAHYDROISOQUINOLINE DERIVATIVES HAVING EFFECTS OF PREVENTING AND TREATING DEGENERATIVE AND INFLAMMATORY DISEASES

Provided are 7-hydroxy-6-methoxy-l,2,3,4-tetrahydroisoquinoline derivatives and synthesis methods thereof. The compounds significantly inhibit the production of nitrogen monoxide (NO) and superoxide in an activated microglial cell and expressions of TNF-α, IL- lβ inducive NO synthase and cyclooxygenase-2 genes. They also prevent NF-kB shift to a nucleus, decrease reactive oxygen species (ROS), inhibit expression of GTP cyclohydrolase I gene and over-production of tetrahydrobiopterin (BH 4 ), and protect dopaminergic neurons from injury due to activated microglial cells. Consequently, the compounds are effective in treating inflammatory and neurodegenerative diseases.

Syntheses of tetrahydroisoquinoline derivatives that inhibit NO production in activated BV-2 microglial cells

Seventeen tetrahydroisoquinoline derivatives were designed, synthesized and evaluated for inhibition of NO production in lipopolysaccharide-stimulated BV-2 microglial cells. Compounds 5a, 9c and 11a potently attenuated NO production by >60%, and 5a and 11

2 -PHENYLETHYLAMINO DERIVATIVES AS CALCIUM AND/OR SODIUM CHANNEL MODULATORS

2-Phenylethylamino substituted carboxamide derivatives of formula (I); wherein J, W, R, R0 R1, R2, R3, and R4 have the meanings as defined in the specification and pharmaceutically acceptable salts th

Glyoxyl acid amides, method for producing them and their use for controlling harmful organisms

The invention relates to novel gloyoxylic acid amides, to a process for their preparation and to their use for controlling harmful organisms.

O2-Cu2+-ASCORBIC ACID: A NOVEL OXIDATION SYSTEM FOR THE HIGHLY SELECTIVE O-DEALKYLATION OF 2-ALKOXYPHENOLS

The novel oxidation system "O2-Cu2+-ascorbic acid" is a selective reagent for the oxidative O-dealkylation of 2-alkoxyphenols and affords catechols in good yield.KEYWORDS - O-dealkylation; ascorbic acid; copper ion; oxidation; 2-alkoxyphenol; vanillin; dopamine; guaiacol; catechol