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An efficient and scalable preparation of the thyroid hormone analogue O-[3-iodo-4-(sulfooxy)phenyl]-3,5-diiodo-l-tyrosine sodium salt (T3-sulfate, 1) is reported. The synthesis involved monoiodination of O-(4-hydroxyphenyl)-3,5-diiodo-l-tyrosine to give liothyronine (2) which was sulfated with chlorosulfonic acid in N,N-dimethylacetamide. Crude T3-sulfate was initially purified by chromatography on polystyrene resin Amberlite XAD 1600 and then crystallized with ethanol. This strategy was scaled-up to give a process suitable for the production of kilogram quantities of API, needed to support preclinical and clinical studies.

An innovative synthetic pathway for the synthesis of chalcones is proposed, using the chemical and environmental advantages of the solvent-free chemistry. The protocol is used for the synthesis of different...