| 主权项 |
1. A process for making a compound of formula (I): the process comprising reacting a compound of formula (II): with lithium diisopropylamide to provide a first intermediate; and reacting the first intermediate with a compound of formula (III): to provide the compound of formula (I), wherein X is selected from oxygen and sulfur; R1 and R2 are each independently selected from —(C1-C6)alkyl and phenyl; or R1 and R2 may join to form a group selected from cyclopentyl, cyclohexyl, and a 5- to 6-membered heterocycloalkyl; R3 is t-butyl or 2,4,6-triisopropylphenyl; R4 is selected from H, —(C1-C6)alkyl, —(C3-C6)cycloalkyl, a bicycloalkyl, a tricyloalkyl, and phenyl; wherein each of the foregoing —(C1-C6)alkyl, —(C3-C6)cycloalkyl, bicycloalkyl, tricyloalkyl, and phenyl R4 groups is optionally substituted by 1 to 3 R6 groups; R5 is selected from t-butyl, phenyl, —C═C(R)-phenyl, and —C≡C-phenyl; wherein each of the foregoing t-butyl, phenyl, —C═C(R)-phenyl, and —C≡C-phenyl of said R5 group is optionally substituted by 1 to 3 R6 groups; or R4 and R5 may join to form a group selected from cyclobutyl, cyclopentyl, cyclohexyl or dihydroindenyl, wherein each of the foregoing cyclobutyl, cyclopentyl, cyclohexyl or dihydroindenyl groups may be optionally substituted by 1 to 3 R6 groups; and/or each of said cyclobutyl, cyclopentyl, cyclohexyl and dihydroindenyl groups may additionally be substituted by a 6-member spirocycloalkyl optionally substituted by 1 to 3 R7 groups; each R6 is independently selected from halo, hydroxyl, —(C1-C6)alkyl, and —O—(C1-C6)alkyl; and each R7 is independently selected from halo, hydroxyl, —(C1-C6)alkyl, and —O—(C1-C6)alkyl. |
