82463-75-0

Upstream product

• 1521-41-1 veratramide 
• 55171-61-4 2-bromo-4,5-dimethoxybenzoyl chloride 
• 5392-10-9 2-bromo-4,5-dimethoxybenzaldehyde 
• 6286-46-0 2-bromo-4,5-dimethoxybenzoic acid 
• 93-07-2 Veratric acid 

Downstream Products

• 128580-95-0 2-bromo-4,5-dimethoxy-N-[(Z)-2-(4-methoxy-phenyl)vinyl]benzamide 
• 1251924-24-9 2-bromo-4,5-dimethoxybenzylamine hydrochloride 
• 1293324-06-7 (2-bromo-4,5-dimethoxybenzyl)carbamic acid tert-butyl ester 
• 1293324-13-6 (2-bromo-4,5-dimethoxybenzyl)(cyclohex-2-enyl)carbamic acid tert-butyl ester 
• 109305-98-8 2-bromo-4,5-dimethoxybenzonitrile 
• 493-49-2 6,7-dimethoxy-3,4-dihydro-2H-isoquinolin-1-one 

Relevant academic research and scientific papers

A versatile approach to 1-oxo-, 1-oxo-3,4-dihydro- and 1,3,4-trioxo isoquinoline alkaloids and first total synthesis of the dimeric 1-oxoisoquinoline alkaloids berbanine and berbidine

We have worked out a very short approach to 1-oxoisoquinoline alkaloids starting from readily available 2-bromobenzamides utilizing a 2-ethoxyvinylboronate as a C2 building block for introduction of the C-3,C-4 unit of the isoquinoline core. TF

Novel nucleocapsid protein-targeting phenanthridine inhibitors of SARS-CoV-2

The COVID-19 pandemic caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is unprecedented in human history. As a major structural protein, nucleocapsid protein (NPro) is critical to the replication of SARS-CoV-2. In this work, 17 NPro-

Phenanthridine Derivative Host Heat Shock Cognate 70 Down-Regulators as Porcine Epidemic Diarrhea Virus Inhibitors

Porcine epidemic diarrhea virus (PEDV) has become increasingly problematic around the world, not only for its hazards to livestock but also due to the possibility that it is a zoonotic disease. Although vaccine therapy has made some progress toward PEDV c

Regio- and Stereoselective Synthesis of Isoindolin-1-ones through BuLi-Mediated Iodoaminocyclization of 2-(1-Alkynyl)benzamides

A simple and straightforward synthesis of isoindolin-1-ones is reported. Exclusive N-cyclization of the amide functional group, an ambident nucleophile, was accomplished for the cyclization of 2-(1-alkynyl)benzamides using n-BuLi-I2/ICl. The methodology works with the primary amide and affords the desired isoindolinones in yields of 38-94%. Interestingly, the isolated products exhibit a Z-stereochemistry across the C=C double bond. The reaction mechanism involving the formation of either a vinylic anion or an intimate ion pair intermediate is proposed.

High-temperature synthesis of amides from alcohols or aldehydes by using flow chemistry

An efficient conversion of aliphatic and aromatic alcohols or aldehydes into the corresponding primary amides was successfully achieved by using flow chemistry. Excellent yields were obtained in very short reaction times, and thus this method offers an efficient alternative to traditional methods for amide formation.

Rapid synthesis and zebrafish evaluation of a phenanthridine-based small molecule library

A Heck cyclisation approach is described for the rapid synthesis of a library of natural product-like small molecules, based on the phenanthridine core. The synthesis of a range of substituted benzylamine building blocks and their incorporation into the library is reported, together with a highly selective cis-dihydroxylation protocol that enables access to the target compounds in an efficient manner. Biological evaluation of the library using zebrafish phenotyping has led to the discovery of compound 20c, a novel inhibitor of early-stage zebrafish embryo development.

Studies on SRN1 Reactions. Part 6: Synthesis of 3-Methyl Derivatives of the Alkaloids Thalactamine, Doryanine, and 6,7-Dimethoxy-N-methyl-1(2H)-isoquinolone

A new, short synthesis of the 3-methyl derivatives (3a-c) of the alkaloids thalactamine, doryanine, and 6,7-dimethoxy-N-methyl-1(2H)-isoquinolone, based upon our previous SRN1 synthesis of isocarbostryril systems, is reported.