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PROCÉDÉ DE PRÉPARATION DE DÉRIVÉS DE PURINE
专利权人:
CYCLACEL LIMITED
发明人:
SKEAD, Ben,WESTWOOD, Robert,LONDESBROUGH, Derek,NORTHERN, Julian,ATHERTON, Chris
申请号:
GBGB2018/050208
公开号:
WO2018/138500A1
申请日:
2018.01.25
申请国别(地区):
GB
年份:
2018
代理人:
摘要:
The present invention relates to a process for preparing a compound of formula [I], said process comprising the steps of: formula [II]+formula [III]−>;formula [I] (i) forming a reaction mixture comprising (a) a compound of formula [II], (b) a compound of formula [III] and (c) 1,2-propanediol or polyethylene glycol, or a mixture thereof, and optionally (d) a base; (ii) heating said reaction mixture to a temperature of at least about 150°C to form a compound of formula [I]; (iii) isolating said compound of formula [I]; and (iv) optionally converting said compound of formula [I] into salt form; wherein: R1 and R2 are each independently H, alkyl or haloalkyl; R3 and R4 are each independently H, alkyl, haloalkyl or aryl; R5 is alkyl, alkenyl, cycloalkyl or cycloalkyl-alkyl, each of which may be optionally substituted with one or more OH groups; R6 is selected from cyclopropylamino, cyclopropylmethylamino, cyclobutylamino, cyclobutylmethylamino and formula (A) where one of X, Y and Z is N and the remainder are CR9; R7, R8 and each R9 are independently H, alkyl or haloalkyl, wherein at least one of R7, R8 and R9 is other than H. Further aspects of the invention relate to a highly diastereoselective process for the preparation of compounds of formula [III], a process for preparing intermediates of formula [II], and other intermediates useful in the synthesis of compounds of formula [I], and to a process for preparing the crystalline tartrate salt and free base of compounds of formula [I].La présente invention concerne un procédé de préparation d'un composé de formule [I], ledit procédé comprenant les étapes consistant à : formule [II] + formule [III] −>; formule [I] (i) former un mélange réactionnel comprenant (a) un composé de formule [II], (b) un composé de formule [III] et (c) du 1,2-propanédiol ou du polyéthylène glycol, ou un mélange de ceux-ci, et éventuellement (d) une base ; (ii) chauffer ledit mélange réactionnel à une température d'au moins environ 150 °C pour
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