Process for the preparation of velpatasvir
The present disclosure provides a process for the preparation of velpatasvir intermediates. The intermediates may be further converted to velpatasvir or pharmaceutically acceptable salts thereof.
1. A process for the preparation of a compound of formula 5, comprising:
a. reacting a compound of formula 2 with a Grignard reagent to get a compound of formula 4; and
b. treating the compound of formula 4 with a halogenating agent to get a compound of formula 5,
wherein each X is independently selected from the group consisting of —F, —Cl, —Br, and —I.
2. The process according to claim 1 , wherein the halogenating agent is selected from the group consisting of N-bromosuccinimide, N-chlorosuccinimide, N-iodosuccinimide, and liquid bromine.
3. The process according to claim 1 , wherein the treating of the compound of formula 4 with halogenating agent is further performed in the presence of benzoyl peroxide.
4. The process according to claim 1 , further comprising:
a. reacting the compound of formula 5 with a compound of formula 6 to get a compound of formula 7; and
b. cyclizing the compound of formula 7 to get a compound of formula 8,
wherein each X is independently selected from the group consisting of —F, —Cl, —Br, and —I.
5. The process according to claim 1 , further comprising converting the compound of formula 5 into velpatasvir.
6. The process according to claim 4 , further comprising converting the compound of formula 8 into velpatasvir.
7. The process according to claim 5 further comprising converting velpatasvir into a pharmaceutically acceptable salt of velpatasvir.
8. The process according to claim 6 further comprising converting velpatasvir into a pharmaceutically acceptable salt of velpatasvir.