[摘要]：The synthesis of 2-mercapto-4-(pyrrolidin-1-yl)pyridine derivs. starting from 2-bromo-4-(pyrrolidin-1-yl)pyridine-3-carbonitrile (I) is described. The desired derivs. of 2-(phenylthio)-4-(pyrrolidin-1-yl)pyridine-3-carbonitrile were obtained via the reaction of I with suitable thiophenols, while the reaction with benzyl mercaptan gave a related thiobenzyl deriv. Alternatively, compd. I was transformed into 2-mercapto-4-(pyrrolidin-1-yl)pyridine-3-carbonitrile (II). The reaction of II with chloroacetic acid or chloroacetone derivs. gave related products of mercapto group substitution. The latter compds. could be cyclized via the Thorpe-Ziegler reaction to related 3-amino-4-(pyrrolidin-1-yl)thieno[2,3-b]pyridine derivs. The reaction of II with sodium hydroxylamino-O-sulfonate gave the related aminosulfanyl deriv. Selected products were screened for bacteriostatic and antituberculosis activity, and some of them exhibited significant activity.
