Carboxylic acids primary aminomethylation

In an opposite manner to bases such as 1 and 2 in terms of reactivity, polymer-supported tosyl chloride equivalent 14 is able to capture alcohols as polymer-bound sulfonates 15, which are released as secondary amines, sulfides and alkylated imidazoles with primary amines, thiols and imidazoles as nucleophiles in a substitution process (Scheme 6) [24]. This technique has further been extended for the preparation of tertiary amines [25] and esters [26]. Excess of amine was scavenged by polymer-supported isocyanate 16 [27, 28] while excess of carboxylic acid was removed by treatment with aminomethylated polystyrene 17. 

Miscellaneous - Specific amino acids have been studied for anti-inflammatory activity. Thus, the combination of calcium D,L-aspartate/indometha-cin has been repor gd to be effective in primary chronic polyarthritis Dilauroyl-L-lyslne and trans U-aminomethyl-cyclohexane-l-carboxylic acid (tranexamic acid) have anti-inflammatory properties. The activity of tranexamic acid was not attributed to anti-plasmin action. Detailed pharmacology on SKF 17,910-A (X) has been published. This anti-inflammatory and diuretic agent shares some biological properties with glucocorticoids. 

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