摘要 |
<p>Sulphonamidepyrimidine derivs. (I): (where R1, R3 and R4 are H, 1-5C, n- or iso-alkyl, or F, Cl, Br or I; R2 is H or 1-5 C n- or iso-alkyl and n is zero or 1) have higher blood-sugar lowering activity than "Tolbutamide" (RTM). (I) are prepd. by reacting a 2-amino-pyrimidine : with a benzenesulphonyl R4-C6H4-SO2X (II) (where x is Cl or Br or a reactive gp. capable of forming -SO2NH, such as a mixed acid anhydride, ester or cyanide gp.) in opt. presence of an inert solvent and in presence of an acylation catalyst. Prepn. of (III) is also claimed.</p> |