[EN] PROCESS FOR THE PREPARATION OF MORPHINAN-6-ONE COMPOUNDS<br/>[FR] PROCÉDÉ DE PRÉPARATION DE COMPOSÉS MORPHINAN-6-ONES
申请人:JOHNSON MATTHEY PLC
公开号:WO2015015147A1
公开(公告)日:2015-02-05
The present provides a process for preparing a compound of formula (3), the process comprising the steps of: (a) providing an aqueous acidic solution comprising a compound of formula (1) and, as an impurity, a compound of formula (2); and (b) treating the aqueous acidic solution of step (a) such that the compound of formula (2) dehydrates to form a compound of formula (1) and the compound of formula (1) is reduced to form an aqueous acidic solution of the compound of formula (3), wherein: the treating of step (b) is carried out at one or more temperatures greater than ambient in the presence of a hydrogenation catalyst and hydrogen gas; and wherein for the compounds of formulae (1), (2) and (3): i) R1 is -OH, R2 is-OH and R3-H; or ii) R1 is -OCH3, R2 is -H and R3 -CH3; or iii) R1 is-OH, R2 is-H and R3-CH3; or iv) R1, is -OCH3, R2 is -H and R3 -H; or v) R1, is -OH, R2is-H and R3-H; or vi) R1, is -OCH3, R2 is -OH and R3 -H.
本发明提供了一种制备式(3)化合物的方法,该方法包括以下步骤:(a)提供含有式(1)化合物和式(2)化合物作为杂质的水酸性溶液;和(b)处理步骤(a)中的水酸性溶液,使得式(2)化合物脱水形成式(1)化合物,而式(1)化合物还原形成含有式(3)化合物的水酸性溶液,其中:步骤(b)的处理在氢化催化剂和氢气的存在下,在一个或多个高于环境温度的温度下进行;对于式(1)、(2)和(3)化合物:i)R1为-OH,R2为-OH,R3为H;或ii)R1为-OCH3,R2为H,R3为CH3;或iii)R1为-OH,R2为H,R3为CH3;或iv)R1为-OCH3,R2为H,R3为H;或v)R1为-OH,R2为H,R3为H;或vi)R1为-OCH3,R2为-OH,R3为H。