Technical documentation

The synthesis of t-butyldimethylsilyl cyanoacetate and the reactions of its anion with acyl donors are described. The reagent was found to be the method of choice for the syntheses of α-cyano ketone substrate analogues for carboxypeptidase A. These compounds have been shown to be potent mechanism-based inactivators for the enzyme.

An effective protocol has been developed that allows the smooth protodecarboxylation of diversely functionalized aromatic carboxylic acids within 5−15 min. In the presence of at most 5 mol % of an inexpensive catalyst generated in situ from copper(I) oxide and 1,10-phenanthroline, even nonactivated benzoates were converted in high yields and with great preparative ease.

The invention relates to new industrial products of the general formula ##STR1## a process for the manufacture of these products and their application in hydrometallurgy.

Reaction of 3-substituted isocoumarins (la-h) with excess of sodium borohydride in methanol gave the corresponding 2-(2-(hydroxymethyl)phenyl)ethanol derivatives (2a-h). Antimicrobial activities of synthesized compounds were measured, using Gram-negative (Escherichia coli, Salmonella typhi, Proteus mirabilis) and Gram-positive bacteria (Bacillus cereus, Staphylococcus aureus).