150191-66-5

Upstream product

• 121171-08-2 5-bromo-2,2-diphenyl-1,3-benzodioxole 
• 2051-90-3 Dichlorodiphenylmethane 
• 139-85-5 3,4-dihydroxybenzaldehyde 
• 65638-94-0 2,2-diphenylbenzo(1,3-dioxole)-5-carboxylic acid methyl ester 
• 2150-43-8 3,4-dihydroxybenzoic acid methyl ester 
• 70006-59-6 2,2-Diphenyl-1,3-benzodioxol-5-methanol 

Downstream Products

• 213984-35-1 N-(2,2-Diphenyl-benzo[1,3]dioxol-5-ylmethyl)-2,2,2-trifluoro-N-[2-(4-hydroxy-phenyl)-ethyl]-acetamide 

Relevant academic research and scientific papers

Synthesis, evaluation and molecular modelling of piceatannol analogues as arginase inhibitors

Arginase is involved in a wide range of pathologies including cardiovascular diseases and infectious diseases whilst it is also a promising target to improve cancer immunotherapy. To date, only a limited number of inhibitors of arginase have been reported. Natural polyphenols, among them piceatannol, are moderate inhibitors of arginase. Herein, we report our efforts to investigate catechol binding by quantum chemistry and generate analogues of piceatannol. In this work, we synthesized a novel series of amino-polyphenols which were then evaluated as arginase inhibitors. Their structure-activity relationships were elucidated by deep quantum chemistry modelling. 4-((3,4-Dihydroxybenzyl)amino)benzene-1,2-diol3tdisplays a mixed inhibition activity on bovine and human arginase I with IC50(Ki) values of 76 (82) μM and 89 μM, respectively.

Extensive structure modification on luteolin-cinnamic acid conjugates leading to BACE1 inhibitors with optimal pharmacological properties

BACE1 inhibitory conjugates derived from two natural products, luteolin (1) and p-hydroxy-cinnamic acid (2), were subjected to systematic structure modifications, including various positions in luteolin segment for conjugation, different linkers (length, bond variation), as well as various substitutions in cinnamic acid segment (various substituents on benzene, and replacement of benzene by heteroaromatics and cycloalkane). Optimal conjugates such as 7c and 7k were chosen on the basis of a series of bioassay data for further investigation.

Oxidative Intramolecular Phenolic Coupling Reaction Induced by a Hypervalent Iodine(III) Reagent: Leading to Galanthamine-Type Amaryllidaceae Alkaloids

By extending our oxidative phenol-coupling reactions using a hypervalent iodine(III) reagent, a versatile synthetic procedure for the galanthamine-type Amaryllidaceae alkaloids was accomplished. The first total synthesis of (±)-sanguinine and the total syntheses of (±)-galanthamine, (±)- narwedine, (±)-lycoramine, and (±)-norgalanthamine were also successfully carried out.

Cephalosporin derivatives

Cephalosporin derivatives have the formula STR1 wherein Z1, Z2, X, Y, P, Q, m, n and p are as defined in the following text. Also described are the readily hydrolyzable esters and pharmaceutically compatible salts of these compounds, and hydrates of compounds of formula I, their esters and salts. Processes are provided for manufacture and pharmaceutical preparations which contain these compounds. Intermediates from the manufacture of these compounds are described, as is the use of the compounds in the control of illnesses and for the manufacture of the aforementioned preparations.