[EN] PROCESSES FOR THE PREPARATION OF AZD5363 AND NOVEL INTERMEDIATE USED THEREIN<br/>[FR] PROCÉDÉS DE PRÉPARATION D'AZD5363 ET NOUVEL INTERMÉDIAIRE UTILISÉ DANS CES DERNIERS
申请人:ASTRAZENECA AB
公开号:WO2015181532A1
公开(公告)日:2015-12-03
There is provided a process for the preparation of AZD5363, or a salt of AZD5363, comprising: (a) the reaction of 8-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-3-oxa-l,8- diazaspiro[4.5]decane-2,4-dione: or a salt thereof, with (S)-3-amino-3-(4-chlorophenyl)propan-1-ol, or a salt thereof, in the presence of base; and (b) either isolating AZD5363 or isolating AZD5363 as a salt. 8-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-3-oxa-1,8-diazaspiro[4.5]decane-2,4-dione is provided and is prepared by reacting 4-(alkyloxycarbonylamino)-1-(7H-pyrrolo[2,3-d]pyrimidin-4- yl)piperidine-4-carboxylic acid, or a salt thereof, with a cyclising agent
提供一种制备AZD5363或其盐的方法,包括:(a)将8-(7H-吡咯并[2,3-d]嘧啶-4-基)-3-氧杂-1,8-二氮杂螺[4.5]癸烷-2,4-二酮或其盐与(S)-3-氨基-3-(4-氯苯基)丙醇或其盐在碱存在下反应;(b)隔离AZD5363或作为盐隔离AZD5363。提供8-(7H-吡咯并[2,3-d]嘧啶-4-基)-3-氧-1,8-二氮杂螺[4.5]癸烷-2,4-二酮,通过将4-(烷氧羰基氨基)-1-(7H-吡咯并[2,3-d]嘧啶-4-基)哌啶-4-羧酸或其盐与环化剂反应制备。