Ad una soluzione del composto 17b-d (10.28 mmol) in CHCl3 a 0°C si aggiunge goccia a goccia SOCl2 (1.223 g; 10.28 mmol; 0.74 ml). La miscela è stata lasciata sotto agitazione per 12 h a t.a., e trascorso tale periodo, è stata lavata con H2O. La fase organica è stata essiccata e concentrata per evaporazione a p.r. ed il prodotto è stato utilizzato per la reazione successiva senza ulteriore purificazione.
2,3-Dimetossibenzilcloruro (10b)
OCH3 OCH3 Cl 10b RESA: 85% 1 H NMR (CDCl3): δ 3.87 (s, 3H, OCH3); 3.96 (s, 3H, OCH3); 4.57 (s, 2H, CH2); 6.85-7.07 (m, 3H, Ar) ppm.61
3,4-Dimetossibenzilcloruro (10c)
OCH3 OCH3 Cl 10c RESA: 70% 1 H NMR (CDCl3): δ 3.88 (s, 3H, OCH3); 3.90 (s, 3H, OCH3); 4.57 (s, 2H, CH2); 6.79-6.88 (m, 1H, Ar); 6.92-6.98 (m, 2H, Ar) ppm. 3,4,5-Trimetossibenzilcloruro (10d)
OCH3 OCH3 Cl H3CO 10d RESA: 84% 1 H NMR (CDCl3): δ 3.88 (s, 3H, OCH3); 3.90 (s, 3H, OCH3); 4.57 (s, 2H, CH2); 6.80-6.84 (m, 1H, Ar); 6.91-6.96 (m, 2H, Ar) ppm.63
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Struttura Pag 3
Localizzazione Pag 5
Barriera Ematoencefalica Pag 6
Barriera Sangue-Fluido Cerebrospinale Pag 8
Placenta Pag 9
Fattori di regolazione Pag 11
P-pg e le malattie neurodegenerative Pag 13
Meccanismo d’azione Pag 15
Substrati-Modulatori-Inibitori Pag 16
Substrati e Modulatori Pag 16
Inibitori Pag 17
P-gp nella chemioterapia Pag 23
Inibitori di prima generazione Pag 23
Inibitori di seconda generazione Pag 24
Inibitori di terza generazione Pag 25