The invention belongs to the technical field of
medicine preparation, and particularly relates to a synthesis method and an intermediate of rosmeltirol. The method comprises the following steps: (1) mixing SM1, organic
monobasic acid and inorganic acid in proportion, stirring and dissolving, dropwise adding a
sodium salt solution, and then adding SM2 and a
carboxylate solution for reaction to prepare an intermediate 1; (2) dissolving the intermediate 1 in an
amide compound, adding
potassium salt, heating for reaction, and purifying to obtain an intermediate 2; (3) dissolving the intermediate 2 in
aromatic hydrocarbon, adding
boride, and performing deprotection and purification to obtain an intermediate 3; and (4) dissolving the intermediate 3 in an organic
sulfide, then adding SM3 and inorganic salt, and carrying out heating reaction and purification to obtain the rosimeltirome. The method provided by the invention has the characteristics of concise, efficient and safe synthesis of the rosmeltirol, reduces by-products, is helpful for improving the purity and stability of the product, avoids the use of expensive
Grignard reagent and complex purification steps, and is more suitable for large-scale industrial production.