[EN] PROCESS FOR THE PREPARATION OF ENANTIOMERICALLY AND DIASTEREOMERICALLY ENRICHED CYCLOBUTANE AMINES AND AMIDES [FR] PROCÉDÉ DE PRÉPARATION D'AMINES ET D'AMIDES DE CYCLOBUTANE ÉNANTIOMÉRIQUEMENT ET DIASTÉRÉOMÉRIQUEMENT ENRICHIS
The present invention relates to compounds of formula I
wherein A, n, R
1a
to R
1e
and R
2
to R
5
are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.
Process for the preparation of enantiomerically and diastereomerically enriched cyclobutane amines and amides
申请人:SYNGENTA PARTICIPATIONS AG
公开号:US11053188B2
公开(公告)日:2021-07-06
The present invention relates to a process for the preparation of enantiomerically and diastereomerically enriched cyclobutane amines and amides by reacting (a) cyclopropylcarbonitrile to a cyclopropylcarbaldehyde, (b) further reacting to a cyclobutanone, or (d′) further reacting to an enamide, (c) further reacting to enantiomerically and diastereomerically enriched cyclobutane amines, or (d) further reacting to an enamide and (e) to an enantiomerically and diastereomerically enriched cyclobutylamide to obtain (f) an enantiomerically and diastereomerically enriched cyclobutane amine, and (g) further reacting to an enantiomerically and diastereomerically enriched cyclobutane amide.