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    • 8. 发明申请
    • PROCESS FOR SYNTHESISING HELIOTROPINE AND ITS DERIVATIVES
    • 合成有机化合物及其衍生物的方法
    • WO2005042512A1
    • 2005-05-12
    • PCT/EP2004/052710
    • 2004-10-28
    • ENDURA S.P.A.BORZATTA, ValerioCAPPARELLA, ElisaGOBBI, CarlottaPOLUZZI, Elisa
    • BORZATTA, ValerioCAPPARELLA, ElisaGOBBI, CarlottaPOLUZZI, Elisa
    • C07D317/54
    • C07D317/54
    • A new high-yield, easily industrialized process for synthesising compounds of formula (IV), in which X 1 and X 2 , the same or different, are linear or branched C1-C8 alkyls, n and m are 0,1 or 2, with the proviso that n and m are not simultaneously 0; or (OX 1 )n and (OX 2 )m taken together form an O-T-O group where T is chosen from -CH 2 -, -CH 2 CH 2­ , -CH 2 CH 2 CH 2 -, -C(CH 3 ) 2 -. The process comprises treating a chloromethyl derivative (I) with an alkaline acetate to form the intermediate acetylderivative (II); the intermediate (II) is to hydrolysed to form the alcohol (III); the alcohol (III) is then oxidised in the presence of air and catalysts to obtain the desired derivative (IV). The process runs its course within a short period of time, with high yields and high selectivity; in addition, the process does not require purification and separation of the intermediates and can therefore be favourably conducted in a single batch.
    • 合成式(IV)化合物的新的高产率,易于工业化的方法,其中X1和X2相同或不同,为直链或支链C1-C8烷基,n和m为0,1或2,其中 条件是n和m不同时为0; 或(OX 1)n和(OX 2)m一起形成O-T-O基团,其中T选自-CH 2 - , - CH 2 CH 2,-CH 2 CH 2 CH 2 - , - C(CH 3)2 - 。 该方法包括用碱性乙酸盐处理氯甲基衍生物(I)以形成中间体乙酰衍生物(II); 中间体(II)被水解形成醇(III); 然后在空气和催化剂的存在下将醇(III)氧化以获得所需的衍生物(IV)。 该过程在短时间内运行,产量高,选择性高; 此外,该方法不需要中间体的纯化和分离,因此可以在单次批次中有利地进行。