| 主权项 |
1. A method of making a compound of formula (I), or a stereoisomer thereof, a diastereomer thereof, or a salt of any one of foregoing, comprising:
(A) reacting a compound of formula (II), or a stereoisomer or a salt thereof, with R1CO2H to form a compound of formula (III); and (B) reacting the compound of formula (III), or a stereoisomer or a salt thereof, with HNR4aR4b to form the compound of formula (I):wherein:
each of R1 and R2 is independently C1-4 alkyl; R3 is H or C1-4 alkyl; HNR4aR4b is a drug molecule having an amino moiety; R4a and R4a are groups of the drug molecule attached to the amino moiety; each of R5a, R5b, R5c, R5d, and R5e is independently selected from H, halo, C1-4 alkyl, halo C1-4 alkyl, phenyl, —C(O)O—C1-4 alkyl, —C(O)—C1-4 alkyl, —S(O)—C1-4 alkyl, CN, —C(O)—NR6aR6b, substituted or unsubstituted C1-4 alkoxy, and substituted or unsubstituted phenoxy; provided that at least one of R5a, R5b, R5c, R5d, and R5e is other than H; or any two adjacent R5a, R5b, R5c, R5d, and R5e are joined together to form a carbocycle or heterocycle; each R6a and R6b is independently H, or C1-4 alkyl; or R6a and R6b together with N they are attached to form heterocycle; and X is a leaving group. |
