| 主权项 |
1. A process for the preparation of a compound of formula (I)wherein
R1 is selected from the group consisting of C1-4alkyl and C3-10cycloalkyl; m is an integer from 1 to 2; R2 is selected from the group consisting of —OCHR3R4 and —Z—Ar; R3 is hydrogen and R4 is a C3-10cycloalkyl or heterocycloalkyl ring; wherein the C3-10cycloalkyl or the heterocycloalkyl ring is unsubstituted or substituted with —C1-4alkyl or acetyl; alternatively, R3 and R4 are taken together with the carbon to which they are attached to form a C3-10cycloalkyl or heterocycloalkyl ring; wherein the C3-10cycloalkyl or the heterocycloalkyl ring is unsubstituted or substituted with —C1-4alkyl or acetyl; Z is selected from the group consisting of S and O; Ar is a phenyl or heteroaryl; wherein the phenyl or heteroaryl is unsubstituted or substituted with one, two, or three R5 substituents; wherein each R5 substituent is independently selected from the group consisting of halogen, —C1-4alkyl, —OH, —OC1-4alkyl, —SC1-4alkyl, —CN, —CONRaRb, and —NO2; and wherein Ra and Rb are each independently —H or —C1-4alkyl;or a pharmaceutically acceptable salt, a pharmaceutically acceptable prodrug, or a pharmaceutically active metabolite thereof; comprisingreacting a compound of formula (V) with a compound of formula (VI), wherein LG1 is a first leaving group and LG2 is a second leaving group, in the presence of a base, in an organic solvent; to yield the corresponding compound of formula (VII); reacting the compound of formula (VII) with an aldehyde or ketone derivative of the desired R1 substituent group; in the presence of a reducing agent; in an organic solvent; to yield the corresponding compound of formula (X); reacting the compound of formula (X) with a compound of formula (XII); in the presence of a first inorganic base; in an organic solvent; or reacting the compound of formula (X) with a compound of formula (XIII); in the presence of a second inorganic base; in an organic solvent;to yield the corresponding compound of formula (I). |
