Syntesis of Ametoctradin - Methods - Method 1 - Non-elaborate posts - Post 2

 

 

The next stage involves the introduction of the exocyclic amino group at the 7-position. This can be achieved through nucleophilic substitution of a leaving group, such as chlorine, on the heterocycle by ammonia or an amine source. The result is the 7-amine triazolopyrimidine, which forms the pharmacophore essential for bioactivity at the Qo-site of cytochrome bc1.

Following this, the ethyl substituent at the 5-position and the octyl substituent at the 6-position are installed via alkylation reactions, often through the use of Grignard reagents or organolithium chemistry, depending on precursor availability. The long C8 side chain, the octyl group, is particularly important, as it enhances lipophilicity and enables the fungicide to embed within the hydrophobic regions of the mitochondrial membrane.

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