| 摘要 |
<p>Isoquinoline derivs. used to lower blood-sugar content. These isoquinoline derivs. (I): (where R1 is H, Cl, Br or 1-4C alkoxy and R2 is cyclohexyl or adamantyl-1) or their alkali salts, are prepd. by (a) ring-closure of (II): (where one A or B is -NH-CH2-CH2-C6H4-p-SO2-NH-CO-NH-R2 and the other group A or B is OH or a reactive gp.); or (b) by replacing S by O in isoquinoline thiourea; or (c) by methylating (I) where CH3 is H; or (d) by reacting sulphonylisocyanate deriv. with an amine H2N-R2; or (e) by reacting sulphonamide deriv. with Y-CO-NH-R2 (where Y is halogen, amino, OH or SH opt. substd. by (ar)alkyl or aryl) in presence of a base; or (f) by reacting a sulphonyl halide deriv. with a parabanic acid (III): or (g) by reacting with amine H2N-R2 or (h) by dealkylating a substd. urea deriv. using HCl, or (i) in prepn. of (I) where R1 is 1-4C alkoxy, alkylating a 7-hydroxyisoquinoline deriv.</p> |
