| 主权项 |
1. A method for preparing the compound of Formula I:the method comprising:
forming a reaction mixture comprising a compound of Formula II: a silane reducing agent,a catalyst, anda solvent, under conditions suitable to prepare the compound of Formula I,wherein
X is bromo or iodo, R1 is selected from the group consisting of hydrogen, halogen, C1-C3 alkyl, C2-C4 alkene, C2-C4 alkyne, C3-C6 cycloalkyl, and —CN, each R2 and R3 is independently selected from the group consisting of hydrogen, halo, hydroxy, C1-C3 alkyl, C2-C4 alkenyl, C1-C3 alkoxy, C1-C3 alkyl-hydroxy, C3-C6 cycloalkyl, (C1-C3 alkoxy)C1-C3 alkyl, (C1-C3 haloalkoxy)C1-C3 alkyl, (C2-C4 alkenyloxy)C1-C3 alkyl, (C2-C4 alkynyloxy)C1-C3 alkyl, (C3-C6 cycloalkoxy)C1-C3 alkyl, C1-C3 hydroxyalkoxy, C3-C6 cycloalkoxy, C3-C6 heterocycloalkoxy, (C1-C3 alkoxy)C1-C3 alkoxy, (C1-C3 haloalkoxy)C1-C3 alkoxy, (C2-C4 alkenyloxy)C1-C3 alkoxy, (C2-C4 alkynyloxy)C1-C3 alkoxy, (C3-C6 cycloalkoxy)C1-C3 alkoxy, (C3-C6 heterocycloalkoxy)C1-C3 alkoxy, (C3-C6 cycloalkyl)C1-C3 alkoxy, (C3-C6 cycloalkyl)C2-C4 alkenyloxy, (C3-C6 cycloalkyl)C2-C4 alkynyloxy, —C(O)H, —C(O)OH, and —C(O)O—C1-C3 alkyl, wherein at least one R3 is selected from the group consisting of C1-C3 alkoxy, C1-C3 hydroxyalkoxy, C3-C6 cycloalkoxy, C3-C6 heterocycloalkoxy, (C1-C3 alkoxy)C1-C3 alkoxy, (C1-C3 haloalkoxy)C1-C3 alkoxy, (C2-C4 alkenyloxy)C1-C3 alkoxy, (C2-C4 alkynyloxy)C1-C3 alkoxy, (C3-C6 cycloalkoxy)C1-C3 alkoxy, (C3-C6 heterocycloalkoxy)C1-C3 alkoxy, (C3-C6 cycloalkyl)C1-C3 alkoxy, (C3-C6 cycloalkyl)C2-C4 alkenyloxy and (C3-C6 cycloalkyl)C2-C4 alkynyloxy; each R4 is independently selected from the group consisting of hydrogen, halo, —OR4a, C1-C3 alkyl, C2-C4 alkenyl, C1-C3 alkoxy, C1-C3 alkyl-hydroxy, C3-C6 cycloalkyl, (C1-C3 alkoxy)C1-C3 alkyl, (C1-C3 haloalkoxy)C1-C3 alkyl, (C2-C4 alkenyloxy)C1-C3 alkyl, (C2-C4 alkynyloxy)C1-C3 alkyl, (C3-C6 cycloalkoxy)C1-C3 alkyl, C1-C3 hydroxyalkoxy, C3-C6 cycloalkoxy, C3-C6 heterocycloalkoxy, (C1-C3 alkoxy)C1-C3 alkoxy, (C1-C3 haloalkoxy)C1-C3 alkoxy, (C2-C4 alkenyloxy)C1-C3 alkoxy, (C2-C4 alkynyloxy)C1-C3 alkoxy, (C3-C6 cycloalkoxy)C1-C3 alkoxy, (C3-C6 heterocycloalkoxy)C1-C3 alkoxy, (C3-C6 cycloalkyl)C1-C3 alkoxy, (C3-C6 cycloalkyl)C2-C4 alkenyloxy, (C3-C6 cycloalkyl)C2-C4 alkynyloxy, —C(O)H, —C(O)OH, and —C(O)O—C1-C3 alkyl, wherein R4a is selected from the group consisting of hydrogen and a silyl group; wherein at least one R4 is —OR4a; ring C is selected from the group consisting of an aryl and a heteroaryl, ring D is absent or selected from the group consisting of an aryl and a heteroaryl, subscript n is an integer from 1 to 4, wherein the alkyl, alkoxy, cycloalkyl, alkenyloxy, alkynyloxy, cycloalkoxy, hydroxyalkoxy, and heterocycloalkoxy groups or portions thereof may optionally be partially or completely fluorinated, and one or more hydrogen atoms optionally may be replaced with deuterium. |
