摘要 |
The present invention relates to processes and intermediates useful for the manufacture of spiroindolone compounds such as (1′R,3′S)-5,7′-dichloro-6′-fluoro-3′-methyl-2′,3′,4′,9′-tetrahydrospiro[indoline-3,1′-pyrido[3,4-b]indol]-2-one and salts and hydrates and solvates thereof. |
主权项 |
1. A process for preparing a compound of formula (II), or a salt or solvate or hydrate thereof, comprising converting a compound of formula (I) to compound of formula (II), or a salt, solvate or hydrate thereof, wherein:
the dashed line is a bond or absent;A is selected from C═O and C═NH; or when the dashed line is a dou Ole bond A-R8 is: Ra is C1-6 alkyl;R1 is H, —CH3, R4 and R7 are each, independently, H or —Cl;R5 is H, —OH, —CH3, —OCH3, —F, —Cl, —CF3 or —CN;R6 is H, —OH, —OCH3, —F or —Cl;R8 is H, —CH3, —CH2CH3, —CH2OH, —CO2H, —CO2CH3, —CO2CH2CH3 or —CF; andn is 1 or 2. |