| 主权项 |
1. A method of preparing a compound of Formula I: comprising reacting a compound of Formula II: in the presence of a metal catalyst and a compound of Formula III:
R2-LG (III), or when R2 is C(O)R6, a compound of Formula IV:
R6═C═O (IV) wherein, R1 is selected from H, C1-10alkyl, C(O)C1-10alkyl, C(O)OC1-10alkyl and PG1; R2 is selected from C(O)R6, C(O)OR6, S(O)R6, SO2R6, P(O)R6R6′, P(O)(OR6)R6′, P(O)(OR6)(OR6′), C(O)NR6R6′ and C(O)SR6; R4 is selected from H, C1-10alkyl, C(O)C1-10alkyl, hydroxyl-substituted C1-10alkyl, and PG3-O-substituted C1-10alkyl; R5 is selected from OH, OC1-10alkyl, OC(O)C1-10alkyl, OC(O)OC1-10alkyl and OPG4; R6 and R6′ are independently selected from C3-10cycloalkyl, C3-10heterocycloalkyl, C3-10cycloalkenyl, C1-20alkyl, C2-20alkenyl, C2-20alkynyl, C6-10aryl and C5-10heteroaryl, each of the latter eight groups being unsubstituted or substituted with one or more substituents independently selected from R7, OR8, SiR7R7′R8, NR8R8′, SR8, S(O)R7, SO2R7, halo, CN and NO2; R7 and R7′ are independently selected from C1-6alkyl, C6-10aryl and C1-6alkyleneC6-10aryl; R8 and R8′ are independently selected from H, PG5, C1-6alkyl, C6-10aryl and C1-6alkyleneC6-10aryl; represents a single or double bond; PG1, PG2, PG3, PG4 and PG5 are independently, a protecting group that is removable after the preparation of the compound of Formula I; and LG is a leaving group, wherein, when (a) R1, R8 and/or R8′ are H; (b) R3 and/or R5 is OH; and/or (c) R4 is hydroxyl-substituted C1-10alkyl, the method further comprises removal of any R2 group in R1, R8, R8′, R3, R5 and/or R4. |
