Br/Mg-exchange reaction using reagents of the general formula R2Mg (R = sBu, Mes). Highly sensitive functional groups, such as triazene or nitro, are tolerated in these exchange reactions, enabling the synthesis of various functionalized (hetero)arene and alkene derivatives after quenching with several electrophiles including allyl bromides, acylchlorides, aldehydes, ketones, and aryl iodides.
在 –78 °C 和 25 °C 之间,通过 I/Mg 或 Br/Mg 交换反应,在甲苯中,在 10 到 120 分钟内,使用以下试剂制备各种多官能化二(杂)芳基和二烯基镁试剂通式 R2Mg (R = sBu, Mes)。在这些交换反应中可以耐受三氮烯或硝基等高度敏感的官能团,在用烯丙基溴、酰氯、醛、酮和芳基碘等多种亲电试剂淬灭后,可以合成各种功能化的(杂)芳烃和烯烃衍生物.
[EN] DOPAMINE D2 RECEPTOR LIGANDS<br/>[FR] LIGANDS DU RÉCEPTEUR D2 DE LA DOPAMINE
申请人:BROAD INST INC
公开号:WO2016100823A1
公开(公告)日:2016-06-23
The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopaminergic activity.
The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopaminergic activity.