Process for preparing idelalisib
AssigneeSynthon BV
InventorsLibor VYKLICKY, Zuzana BEDNAROVA, Radomir SKOUMAL
Life of this patent
Estimating the term…
Abstract
The present invention relates to an improved process of preparation of idelalisib using a solid form of intermediate of formula (2); characterized by XRPD pattern having 2θ values 5.5°, 10.9°, 14.3°, 16.9° (±0.2) the process comprising steps a. Reacting of compound of formula (1); with a chlorinating agent to obtain a product; b. Reacting of the product with (S)-2-((tert-butoxycarbonyl)amino)butanoic acid and a base, wherein pH of the reaction mixture is set between 7.5 and 10 to obtain compound of formula (2); c. Isolating a solid form of compound of formula (2); d. Transforming the compound of formula (2) into idelalisib.
Claims14
A process for preparing idelalisib of formula:
- the process comprising:
- a. Reacting of compound of formula (1):
- with a chlorinating agent to obtain a product;
- b. Reacting of the product with (S)-2-((tert-butoxycarbonyl)amino)butanoic acid and a base, wherein pH of the reaction mixture is set between 7.5 and 10 to obtain compound of formula (2);
- c. isolating a solid form of compound of formula (2);
- wherein the solid compound of formula (2) is characterized by XRPD pattern having 2θ values 5.5°, 10.9°, 14.3°, 16.9° (±0.2);
- and
- d. Transforming the compound of formula (2) into idelalisib.
A solid form of compound of formula (2);
- wherein the solid form is characterized by XRPD pattern having 2θ values 5.5°, 10.9°, 14.3°, 16.9° (±0.2).
Dependencies are inferred from the claim text.