| 摘要 |
3,3-diphenylpropylamines of general formula (I), particularly Fesoterodine, as well as their enantiomers, solvates and salts, can be produced by treating a compound of formula (II) with a chiral alcohol to yield the diastereomeric esters of formula (IV) and (IV′), which can be further transformed into a compound of formula (I), or an enantiomer, solvate or salt thereof, wherein R1 is C1-C8 alkyl; and R2 and R3, independently of one another, represent H or C1-C6 alkyl, or together form a ring of 3 to 7 members with the nitrogen to which they are bound.; |
| 主权项 |
1. A process for preparing a compound of formula (I) or (I′), or a solvate or salt thereof, wherein R1 is C1-C6 alkyl; and R2 and R3, independently of one another, are selected from H and C1-C6 alkyl, or together form a ring of 3 to 7 members with the nitrogen to which they are bound; which comprises
(a) reacting a compound of formula (II), or a solvate or salt thereof, wherein R4 is hydrogen or a hydroxyl protecting group; and R5 is selected from —C(O)Cl, —C(O)Br, —C(O)OH, —C(O)OR′, —C(O)OCOR′ and CN, wherein R′ is selected from C1-C6 alkyl, C1-C6 haloalkyl, aryl and arylalkyl; with an optically active chiral alcohol of formula (III)
R6—OH (III) wherein R6 is a chiral group; to yield compounds of formula (IV) and (IV′), or a solvate or salt thereof, wherein R2, R3, R4 and R6 are as defined previously; and
(b) separating the compound of formula (IV) or (IV′), or a solvate or salt thereof; and(c) converting the compound of formula (IV) or (IV′), or a solvate or salt thereof, into a compound of formula (I) or (I′), respectively, or a solvate or salt thereof. |
