Process for synthesizing heliotropine and its derivatives
    1.
    发明授权
    Process for synthesizing heliotropine and its derivatives 失效
    合成天葵及其衍生物的方法

    公开(公告)号:US07402709B2

    公开(公告)日:2008-07-22

    申请号:US10577846

    申请日:2004-10-28

    IPC分类号: C07C45/90

    CPC分类号: C07D317/54

    摘要: A new high-yield, easily industrialized process for synthesizing compounds of formula (IV), in which X1 and X2, 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 (OX1)n and (OX2)m taken together form an O-T-O group where T is chosen from —CH2—, —CH2CH2, —CH2CH2CH2—, —C(CH3)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.

    摘要翻译: 合成式(IV)化合物的新的高产率,易于工业化的方法,其中相同或不同的X 1和X 2是直链或支链C1 -C 8烷基,n和m为0,1或2,条件是n和m不同时为0; 或(OX 1)n和(OX 2 N)m一起形成OTO基团,其中T选自-CH 2 - , - CH 2 CH 2,CH 2 CH 2 CH 2 - , - 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。

    PROCESS FOR PREPARING 3,4-DIOXO-SUBSTITUTED AROMATIC ALDEHYDES
    2.
    发明申请
    PROCESS FOR PREPARING 3,4-DIOXO-SUBSTITUTED AROMATIC ALDEHYDES 失效
    制备3,4-二氧基取代的芳族醛的方法

    公开(公告)号:US20090062569A1

    公开(公告)日:2009-03-05

    申请号:US11996723

    申请日:2006-07-25

    IPC分类号: C07C45/29

    摘要: A new process for synthesizing 3,4-dioxo-substituted aromatic aldehydes by Oppenauer oxidation of the corresponding benzyl alcohols is described. The process, which specifically uses formaldehyde as hydrogen acceptor, proceeds with unexpectedly high yields and conversion percentages, allowing low cost access to finished and intermediate products of high industrial interest in the field of pharmaceutical products and fragrances.

    摘要翻译: 描述了通过相应的苄醇的Oppenauer氧化合成3,4-二氧代取代的芳族醛的新方法。 特别使用甲醛作为氢受体的方法,出乎意料地高产率和转化率,允许低成本进入医药产品和香料领域具有高工业意义的成品和中间产品。

    Process for preparing 3,4-dioxo-substituted aromatic aldehydes
    3.
    发明授权
    Process for preparing 3,4-dioxo-substituted aromatic aldehydes 失效
    制备3,4-二氧代取代的芳族醛的方法

    公开(公告)号:US07544843B2

    公开(公告)日:2009-06-09

    申请号:US11996723

    申请日:2006-07-25

    IPC分类号: C07C45/29

    摘要: A new process for synthesizing 3,4-dioxo-substituted aromatic aldehydes by Oppenauer oxidation of the corresponding benzyl alcohols is described. The process, which specifically uses formaldehyde as hydrogen acceptor, proceeds with unexpectedly high yields and conversion percentages, allowing low cost access to finished and intermediate products of high industrial interest in the field of pharmaceutical products and fragrances.

    摘要翻译: 描述了通过相应的苄醇的Oppenauer氧化合成3,4-二氧代取代的芳族醛的新方法。 特别使用甲醛作为氢受体的方法,出乎意料地高产率和转化率,允许低成本进入医药产品和香料领域具有高工业意义的成品和中间产品。

    Process for synthesizing heliotropine and its derivatives
    4.
    发明申请
    Process for synthesizing heliotropine and its derivatives 失效
    合成天葵及其衍生物的方法

    公开(公告)号:US20070100167A1

    公开(公告)日:2007-05-03

    申请号:US10577846

    申请日:2004-10-28

    IPC分类号: C07C45/90

    CPC分类号: C07D317/54

    摘要: A new high-yield, easily industrialized process for synthesizing compounds of formula (IV), in which X1 and X2, 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 (OX1)n and (OX2)m taken together form an O-T-O group where T is chosen from —CH2—, —CH2CH2, —CH2CH2CH2—, —C(CH3)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.

    摘要翻译: 合成式(IV)化合物的新的高产率,易于工业化的方法,其中相同或不同的X 1和X 2是直链或支链C1 -C 8烷基,n和m为0,1或2,条件是n和m不同时为0; 或(OX 1)n和(OX 2 N)m一起形成OTO基团,其中T选自-CH 2 - , - CH 2 CH 2,CH 2 CH 2 CH 2 - , - 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。