75803-23-5

Upstream product

• 7417-21-2 2-(3,4-dimethoxyphenyl)ethyl alcohol 
• 6380-23-0 3,4-dimethoxystyrene 
• 120-14-9 3,4-dimethoxy-benzaldehyde 
• 93-40-3 (3,4-Dimethoxyphenyl)acetic acid 
• 124-63-0 methanesulfonyl chloride 

Downstream Products

• 137058-13-0 3-Cyclohexylamino-1-[2-(3,4-dimethoxy-phenyl)-ethyl]-5-methoxy-1,4,5,6-tetrahydro-indol-2-one 
• 503114-36-1 methyl N-3,4-dimethoxyphenethyl-3',4'-bis-(3,4-dimethoxyphenyl)pyrrole-2-carboxylate 
• 64728-23-0 2-(3,4-dimethoxyphenyl)-1-iodoethane 
• 40173-90-8 3,4-dimethoxyphenethyl bromide 
• 1435951-34-0 C₁₅H₂₁NO₄ 
• 1621065-34-6 1-[2-(3,4-dimethoxyphenyl)ethyl]-2,3-dihydroimidazo[1,2-b][1,2,4]benzothiadiazine 5,5-dioxide 
• 1621065-35-7 1-[2-(3,4-dimethoxyphenyl)ethyl]-1,2,3,4-tetrahydropyrimidino[1,2-b][1,2,4]benzothiadiazine 6,6-dioxide 
• 3490-06-0 N-methylhomoveratrylamine 
• 49621-56-9 3-(3,4-dimethoxyphenyl)propanenitrile 
• 864528-55-2 4-(2-azidoethyl)-1,2-dimethoxybenzene 
• 503114-37-2 N-3,4-dimethoxyphenethyl-3',4'-bis-(3,4-dimethoxyphenyl)pyrrole-2-carboxylic acid 
• 266674-78-6 1-(3,4-dimethoxyphenyl)-3-[2-(3,4-dimethoxyphenyl)ethyl]-7,8-dimethoxy-4-oxo-3H-[1]benzopyrano[3,4-b]pyrrole-4-one 

Relevant academic research and scientific papers

NURR1 RECEPTOR MODULATORS

Described herein, inter alia, are Nurr1 receptor modulators and uses thereof. In an aspect is provided a method for treating a disease associated with dysregulation and/or degeneration of dopaminergic neurons in the central nervous system of a subject in need thereof, the method including administering to the subject in need thereof a therapeutically effective amount of a compound described herein.

Convenient Continuous Flow Synthesis of N-Methyl Secondary Amines from Alkyl Mesylates and Epoxides

The first continuous flow process was developed to synthesize N-methyl secondary amines from alkyl mesylates and epoxides via a nucleophilic substitution using aqueous methylamine. A variety of N-methyl secondary amines were produced in good to excellent yields, including a number of bioactive compounds or their precursors. Up to 10.6 g (88% yield) of an N-methyl secondary amine was produced in 140 min process time. The amination procedure included an in-line workup, and the starting mesylate material was also produced in continuous flow from the corresponding alcohol. Finally, an in-line process combining the mesylate synthesis and nucleophilic substitution was developed.

BIOISPIRED PROTEASOME ACTIVATORS WITH ANTIAGEING ACTIVITY

The present invention relates to novel bio-inspired hybrid compounds of formula I which act as proteasome activators and exhibit anti-ageing activity, as well as methods for their synthesis. These hybrid compounds combine the structural features of hydroxytyrosol and the natural antioxidant vitamin E or its bioisosteres in one molecular scaffold. The compounds of formula I, which include structural proteasome activators (activation by stereochemical interaction), can be used in the production of anti-ageing products, such as cosmetic preparations. Additionally, they can be used in conditions and diseases where the proteasome is down-regulated, as well as proteasome-activation control compounds.

Synthesis and Biological Evaluation of N-[2-(4-Hydroxyphenylamino)-pyridin-3-yl]-4-methoxy-benzenesulfonamide (ABT-751) Tricyclic Analogues as Antimitotic and Antivascular Agents with Potent in Vivo Antitumor Activity

Benzopyridothiadiazepine (2a) and benzopyridooxathiazepine (2b) were modified to produce tricyclic quinazolinone 15-18 or benzothiadiazine 26-27 derivatives. These compounds were evaluated in cytotoxicity and tubulin inhibition assays and led to potent inhibitors of tubulin polymerization. N-[2(4-Methoxyphenyl)ethyl]-1,2-dihydro-pyrimidino[2,1-b]quinazolin-6-one (16a) exhibited the best in vitro cytotoxic activity (GI50 10-66.9 nM) against the NCI 60 human tumor cell line and significant potency against tubulin assembly (IC50 0.812 μM). In mechanism studies, 16a was shown to block cell cycle in G2/M phase and to disrupt microtubule formation and displayed good antivascular properties as inhibition of cell migration, invasion, and endothelial tube formation. Compound 16a was evaluated in C57BL/6 mouse melanoma B16F10 xenograft model to validate its antitumor activity, in comparison with reference ABT-751 (1). Compound 16a displayed strong in vivo antitumor and antivascular activities at a dose of 5 mg/kg without obvious toxicity, whereas 1 needed a 10-fold higher concentration to reach similar effects.

Coordination chemistry based approach to lipophilic inhibitors of 1-deoxy-D-xylulose-5-phosphate reductoisomerase

1-Deoxy-D-xylulose-5-phosphate reductoisomerase (DXR) in the non-mevalonate pathway found in most bacteria is a validated anti-infective drug target. Fosmidomycin, a potent DXR inhibitor, is active against Gram-negative bacteria. A coordination chemistry and structure based approach was used to discover a novel, lipophilic DXR inhibitor with an IC50 of 1.4 μM. It exhibited a broad spectrum of activity against Gram-negative and -positive bacteria with minimal inhibition concentrations of 20-100 μM (or 3.7-19 μg/mL).

The application of vinylogous iminium salt derivatives to the synthesis of Ningalin B hexamethyl ether

A vinylogous iminium salt derivative has been used to prepare a 2,3,4-trisubstituted pyrrole synthon in a regioselective, efficient and convenient manner. This pyrrole synthon was subsequently converted to the multidrug-resistant (MDR) reversal agent, Ningalin B hexamethyl ether, via alkylation, hydrolysis and oxidative lactonization steps. This methodology provides an alternative pathway to this important class of pyrrole containing marine natural products.

Substituted naphthalene carboxylic acids

The invention relates to substituted naphthalene carboxylic acid derivatives of the formula STR1 wherein one of R1 and R2 is STR2 and the other is hydrogen, wherein R is hydrogen or lower alkyl, R10 is hydrogen or lower al

Benzothiazepine vasodilators having aralkyl substitution

N-Aminoalkyl 1,5-benzothiazepines of the following formula (I): STR1 for the treatment of angina or hypertension or the prevention of heart attacks in mammals, in particular their use as coronary vasodilators.