| 主权项 |
1. A compound of Formula (I):or a tautomer thereof or a salt of each thereof wherein
R1 is selected from the group consisting of hydrogen, —CO2R11, —COR12, —C(R13)3, an amine protecting group, and R11 is selected from the group consisting of C1-C6 alkyl optionally substituted with 1-3 substituents selected from C6-C10 aryl, C3-C8 cycloalkyl, C2-C10 heteroaryl, C3-C8 heterocyclyl, halo, amino, —N3, hydroxy, C1-C6alkoxy, silyl, nitro, cyano, and CO2H or an ester thereof, C2-C6 alkenyl, C2-C6 alkynyl, C6-C10 aryl, C2-C10 heteroaryl, C3-C8 cycloalkyl, and C3-C8 heterocyclyl, R12 and R13 independently are selected from the group consisting of hydrogen, C1-C6 alkyl optionally substituted with 1-3 substituents selected from C6-C10 aryl, C3-C8 cycloalkyl, C2-C10 heteroaryl, C3-C8 heterocyclyl, halo, amino, —N3, hydroxy, C1-C6alkoxy, silyl, nitro, cyano, and CO2H or an ester thereof, C2-C6 alkenyl, C2-C6 alkynyl, C6-C10 aryl, C2-C10 heteroaryl, C3-C8 cycloalkyl, and C3-C8 heterocyclyl; k is 0, 1, 2, or 3; each R10 is independently a substituent selected from the group consisting of halo, amino, hydroxy, C1-C6 alkoxy, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, cyano, nitro, —N3, and —CO2H or an ester thereof, wherein the alkyl, alkoxy, alkenyl, or the alkylnyl group is optionally substituted with 1-3 substituents selected from the group consisting of keto, halo, amino, hydroxy, cyano, nitro, —N3, phenyl optionally substituted with 1-3 substituents selected from the group consisting of C1-C6 alkyl and C1-C6 alkoxy, and —CO2H or an ester thereof; R20 is hydrogen or C(R20)2 is a keto group; R30 is selected from the group consisting of hydrogen, halo, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, wherein the alkyl, alkenyl, or the alkylnyl group is optionally substituted with 1-3 substituents selected from the group consisting of keto, halo, amino, hydroxy, cyano, nitro, —N3, and —CO2H or an ester thereof; R50 is selected from the group consisting of —O— and N—R51; and R51 is selected from the group consisting of hydrogen and C1-C6 alkyl optionally substituted with 1-3 substituents selected from the group consisting of keto, halo, amino, hydroxy, cyano, nitro, —N3, and —CO2H or an ester thereof; X10 is a leaving group, preferably, halo or —OSO2R71, more preferably bromo or iodo, or is —OH or hydrogen; R4 and R5 independently are selected from the group consisting of hydrogen, halo, C1-C6 alkyl optionally substituted with 1-3 substituents selected from the group consisting of C6-C10 aryl, C3-C8 cycloalkyl, C2-C10 heteroaryl, C3-C8 heterocyclyl, halo, amino, —N3, hydroxy, C1-C6 alkoxy, silyl, nitro, cyano, vinyl, ethynyl, and CO2H or an ester thereof; R2 and R3 are independently selected from hydrogen, —CHO, R6—C(═O)—, R6—CH(OR7)—, provided that at least one of R2 and R3 is hydrogen; or R2 and R3 together with the carbon atom they are bonded to, form a ═CHR6 moiety; R6 is C1-C6 alkyl optionally substituted with 1-3 substituents selected from the group consisting of C6-C10 aryl, C3-C8 cycloalkyl, C2-C10 heteroaryl, or C3-C8 heterocyclyl; R7 is hydrogen or SO2R71; R71 is C1-C6 alkyl optionally substituted with 1-3 substituents selected from the group consisting of C6-C10 aryl, C3-C8 cycloalkyl, C2-C10 heteroaryl, or is C3-C8 heterocyclyl, C6-C10 aryl, C3-C8 cycloalkyl, C2-C10 heteroaryl, or C3-C8 heterocyclyl; wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl, is optionally substituted with 1-3 substituents selected from the group consisting of C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C6-C10 aryl, cycloalkyl, C2-C10 heteroaryl, C3-C8 heterocyclyl, halo, amino, —N3, hydroxy, C1-C6alkoxy, silyl, nitro, cyano, and CO2H or an ester thereof. |
