| 主权项 |
1. A process for preparing a compound of Formula I:or a pharmaceutically acceptable salt thereof, wherein:
R1 is —H, —Cl or —F; R2 is —H or —F; R3 is —C1-4 aliphatic optionally substituted with 1-5 occurrences of R5; R4 is —C1-2 alkyl optionally substituted with 1-3 occurrences of R5; or R3 and R4 are taken together to form a 3-7 membered carbocyclic or heterocyclic saturated ring optionally substituted with 1-5 occurrences of R5; each R5 is independently selected from halogen, —OCH3, —OH, —NO2, —NH2, —SH, —SCH3, —NHCH3, —CN, or unsubstituted —C1-2 aliphatic, or
two R5 groups, together with the carbon to which they are attached, form a cyclopropyl ring; R6 is —H or unsubstituted —C1-2 alkyl; and R7 is a —CH2CR3 or —(CH2)2CR3 wherein each R is independently —H or —F;comprising the step of:
i) reacting a compound of Formula 1 with a hydrochloride salt of a compound Formula 2 in the presence of water, an organic solvent, a base, and a transition metal catalyst to generate a compound of Formula I. |
