108478-56-4

Upstream product

• 109092-63-9 (3'-methoxy-biphenyl-2-yl)-acetic acid ethyl ester 
• 18698-97-0 ortho-bromophenylacetic acid 
• 10365-98-7 3-methoxyphenylboronic acid 
• 109251-54-9 [2-(3-methoxy-phenyl)-cyclohex-1-enyl]-acetic acid ethyl ester 

Relevant academic research and scientific papers

SAR Studies on tetrahydroisoquinoline derivatives: The role of flexibility and bioisosterism to raise potency and selectivity toward P-glycoprotein

The development of P-glycoprotein (P-gp) ligands remains of considerable interest, mostly for investigating the proteins structure and transport mechanism. In recent years, many different generations of ligands have been tested for their ability to modulate P-gp activity. The aim of the present work is to perform SAR studies on tetrahydroisoquinoline derivatives in order to design potent and selective P-gp ligands. For this purpose, the effect of bioisosteric replacement and the role of flexibility have been investigated, and four series of tetrahydroisoquinoline ligands have been developed: (a) 2-aryloxazole bioisosteres, (b) elongated analogues, (c) 2H-chromene, and (d) 2-biphenyl derivatives. The results showed that both 2-biphenyl derivative 20b and elongated derivative 6g behaved as strong P-gp substrates. In conclusion, important aspects for developing potent and selective P-gp ligands have been highlighted, providing a solid starting point for further optimization.

Hydroxyl-substituted phenanthrene derivative synthesis method

The invention relates to a hydroxyl-substituted phenanthrene derivative synthesis method, which includes taking a 2-carboxymethyl biphenyl compound as a raw material; and reacting under the action ofa catalyst to obtain a hydroxyl-substituted phenanthrene derivative, wherein the catalyst comprises one or two of trifluoromethanesulfonic acid or phosphorus pentoxide. Compared with the prior art, the synthesis method has the advantages of the cheap and easily-available catalyst, good universality of functional groups, simple and convenient operation, short reaction time, high reaction yield, mild reaction conditions and the like.