[reaction: see text] A one-step conversion of carboxylic acids to hydroxamic acids under very mild conditions is described. This simple and efficient method has been applied for the synthesis of enantiopure hydroxamate of alpha-amino acids and peptides.

[reaction: see text] A facile conversion of formamides to isonitriles under very mild conditions and microwave irradiation is described. This simple and efficient method has been applied for the synthesis of both aliphatic and aromatic isonitriles in high yields.

The bioactive compounds γ-aminobutyric acid (GABA) and biogenic amines (BA), together with protein-free amino acids, were measured by high-performance liquid chromatography in ewe’s milk cheeses produced in Sardinia with different technological traits. The study included three types of cheese: Pecorino Sardo PDO, Pecorino and Casu Marzu. Farmhouse Casu Marzu and Pecorino showed GABA content (maximum levels: 1001.3 and 378.1 mg 100 g–1 respectively) that had never been found so high in cheese before, suggesting that these types of cheese present ideal conditions to produce GABA. These two types of cheese also showed high levels of BA (their total maximum levels were 1035.7 and 288.0 mg 100 g–1 respectively). Pearson correlation analysis detected significant correlation between GABA and the main BA present in the cheeses (tyramine, cadaverine and putrescine), suggesting that the factors affecting the production of GABA are the same as those influencing BA formation.

A small parallel library of 1,4,5-trisubstituted pyrazoles was prepared in solution using a three-step procedure starting from Meldrum acid. The Meldrum acid was acylated with different acyl chlorides and the products opened with different alcohols and amines to give substituted β-keto esters and β-keto amines. Further reaction with N,N-dimethylformamide dimethylacetal and the final cyclisation were effectivelyThe current development of new methods for the parallel synthesis of libraries of organic molecules has led to renewed interest in a technique in which individual organic molecules are prepared in solution. The advantages of this technique are the standard solution-phase reactivity of the organic molecules, and easy analysis of the reaction using conventional methods without any need for linker chemistry. A particularly important aspect is that the operational time for the preparation of a new library can be shorter than the time necessary to develop a reaction on solid phase. On the other hand, in order to automate the preparation of the library, all the steps must give pure compounds after simple workup, involving exclusively filtration or evaporation under vacuum. To reach this goal, polymersupported reagents have been employed frequently, and recently the developments in the field have been reviewed extensively.[1Ϫ5] The main drawbacks of polymer-assisted solution-phase synthesis are related to the use of polymers that show low loading values and difficulty in swelling in several solvents. Moreover, the prices of several polymersupported reagents or scavengers are sometimes very high.In order to prepare a library of pharmacologically relevant heterocyclic scaffolds with a good level of potential molecular diversity in solution phase, we decided to optimize the synthesis of a trisubstituted pyrazole to obtain a protocol that could be easily automated. We wanted to improve the efficiency of each step to avoid purification and reduce the work-up procedures for a limited number of expensive [a]