Discovery of an Azabicyclo[2.1.1]hexane Piperazinium Salt and Its Application in Medicinal Chemistry via a Rearrangement.
Org Lett
; 26(25): 5318-5322, 2024 Jun 28.
Article
em En
| MEDLINE
| ID: mdl-38888237
ABSTRACT
Herein we report the discovery of an azabicyclo[2.1.1]hexane piperazinium methanesulfonate salt from an unexpected rearrangement reaction in the preparation of ligand-directed degraders (LDDs). This bench-stable compound was found to be a versatile electrophile in a ring-opening reaction with various types of nucleophiles. Its utility as a versatile medicinal chemistry building block is further demonstrated in the synthesis of an LDD compound targeting degradation of the androgen receptor.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Piperazinas
/
Compostos Azabicíclicos
Idioma:
En
Ano de publicação:
2024
Tipo de documento:
Article