2 results about "Ledipasvir" patented technology

The application provides an intermediate for preparing lenacapavir and a preparation method and use thereof, and comprises intermediate compound A and intermediate compound B and a preparation method thereof. In the technical scheme provided by the application, a high-quality lenacapavir intermediate can be obtained, without the need for separation and purification by using a silica gel column, without the need for complicated post-treatment operations, the complicated separation and purification steps are avoided, the waste of raw materials is avoided, the production cost is reduced, and the application is more suitable for industrial production.

The application discloses a preparation method of a Ledipasvir intermediate (S)-5-(tert-butoxycarbonyl)-5-azaspiro[2,4]heptane-6-carboxylic acid and an intermediate compound thereof, and belongs to the technical field of synthesis of pharmaceutical intermediates. The method uses N-tert-butoxycarbonyl glycine and (R)-alpha-methyl benzylamine as starting materials, and generates a diastereoisomer mixture of (S)-3A and (R)-3B through amide condensation and intramolecular N-alkylation ring closure reaction, and obtains the target configuration intermediate compound (S)-3A through solvent recrystallization and mother liquor racemization reaction and recrystallization. Further, (S)-3A is further subjected to one-pot deprotection of double protection groups and amino protection to obtain the target product. The yield of the target intermediate configuration obtained by the application can reach 86.7%, the chiral purity of the product is greater than 99%, the operation is simple, the conditions are mild, the reaction stability is high, the recycling of non-target configuration compounds is realized, and the industrialized production is easy.