INDOLE AHR INHIBITORS AND USES THEREOF
The present invention provides compounds useful as inhibitors of AHR, compositions thereof, and methods of using the same.
1 - 23 . (canceled)
24 . A method of preparing compound I-40:
or a salt thereof, the method comprising a step of reacting compound
or a salt thereof, with compound
or a salt thereof.
25 . The method of claim 24 , further comprising a step of converting compound
or a salt thereof, to compound
or a salt thereof.
26 . The method of claim 25 , further comprising a step of converting compound
or a salt thereof, to compound
or a salt thereof.
27 . The method of claim 26 , further comprising a step of reacting compound
or a salt thereof, with compound
or a salt thereof, to form compound
or a salt thereof.
28 . The method of claim 27 , further comprising a step of converting compound
or a salt thereof, to compound
or a salt thereof.
29 . The method of claim 28 , further comprising a step of converting compound
or a salt thereof, to compound N
or a salt thereof.
30 . The method of claim 29 , further comprising a step of converting compound
or a salt thereof, to compound
or a salt thereof.
31 . The method of claim 24 , wherein compound
or a salt thereof, reacts with compound
or a salt thereof, in a solvent comprising i-PrOH.
32 . The method of claim 24 , wherein compound
or a salt thereof, reacts with compound
or a salt thereof, in presence of compound DIEA.
33 . The method of claim 25 , wherein compound
or a salt thereof, is converted to compound
or a salt thereof, by reacting with compound POCl 3 .
34 . The method of claim 26 , wherein compound
or a salt thereof, is converted to compound
or a salt thereof, by reacting with compound triphosgene.
35 . The method of claim 26 , wherein compound
or a salt thereof, is converted to compound
or a salt thereof, in a solvent comprising 1,4-dioxane and THF.
36 . The method of claim 27 , wherein compound
or a salt thereof, reacts with compound
or a salt thereof, in a solvent comprising xylene.
37 . The method of claim 27 , wherein compound
or a salt thereof, reacts with compound
or a salt thereof, in presence of compound AlMe 3 .
38 . The method of claim 28 , wherein compound
or a salt thereof, is converted to compound
or a salt thereof, in a solvent comprising DCM and TEA.
39 . The method of claim 28 , wherein compound
or a salt thereof, is converted to compound
or a salt thereof, by reacting with compound TFAA.
40 . The method of claim 29 , wherein compound
or a salt thereof, is converted to compound
or a salt thereof, by reacting with compound NH 3 ·H 2 O.
41 . The method of claim 29 , wherein compound
or a salt thereof, is converted to compound
or a salt thereof, by in a solvent comprising THF.
42 . The method of claim 30 , wherein compound
or a salt thereof, is converted to compound
or a salt thereof, by reacting with compound SOCl 2 .
43 . The method of claim 30 , wherein compound
or a salt thereof, is converted to compound
or a salt thereof, in a solvent comprising DMF.
44 . A method of preparing compound I-40:
or a salt thereof, the method comprising steps of:
converting compound
or a salt thereof, to compound
or a salt thereof, by reacting with compound SOCl 2 in a solvent comprising DMF;
converting compound
or a salt thereof, to compound
or a salt thereof, by reacting with compound NH 3 ·H 2 O in a solvent comprising THF;
converting compound
or a salt thereof, to compound
or a salt thereof, by reacting with compound TFAA in a solvent comprising DCM and TEA;
reacting compound
or a salt thereof, with compound
or a salt thereof, in presence of compound AlMe 3 in a solvent comprising xylene, to form compound
or a salt thereof,
converting compound
or a salt thereof, to compound
or a salt thereof, by reacting with compound triphosgene in a solvent comprising 1,4-dioxane and THF;
converting compound
or a salt thereof, to compound
or a salt thereof, by reacting with compound POCl 3 ; and
reacting compound
or a salt thereof, with compound
or a salt thereof, in presence of compound DIEA in a solvent comprising i-PrOH.
45 . A compound selected from the group consisting of:
or a salt thereof.