| 摘要 |
<p>Preparation of 1,3-dihydro-6-methylfuro[3,4-c]pyridin-7-ol derivatives involves: (1) protecting 3-hydroxy and 4-hydroxymethyl groups of pyridoxine to form 3,4-protected pyridoxine; (2) oxidizing 5-hydroxymethyl group in the presence of 2,2,6,6-tetramethyl-1-piperdinyloxy (TEMPO) to form 3,4-protected pyridoxal; (3) adding nucleophile to form adduct; and (4) deprotecting the adduct and cyclo-dehydrating. Preparation of 1,3-dihydro-6-methylfuro[3,4-c]pyridin-7-ol derivatives of formula (I) or their salts involves: (1) protecting 3-hydroxy and 4-hydroxymethyl groups of pyridoxine to form 3,4-protected pyridoxine of formula (ii); (2) oxidizing 5-hydroxymethyl group in (ii) using aqueous sodium hypochlorite in the presence of 2,2,6,6-tetramethyl-1-piperdinyloxy (TEMPO) to form 3,4-protected pyridoxal of formula (iii); (3) adding a nucleophile to the pyridoxal to form an adduct of formula (iv); and (4) deprotecting the adduct and cyclo-dehydrating the 4- and 5-hydroxymethyl substituent of the deprotected adduct to form (I). [Image] R : any atom or group; P1> and P2>protecting group; P1>+P2>one protecting group. ACTIVITY : Hypotensive; Uropathic. MECHANISM OF ACTION : None given.</p> |
