发明申请
- 专利标题: Process for synthesizing heliotropine and its derivatives
- 专利标题(中): 合成天葵及其衍生物的方法
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申请号: US10577846申请日: 2004-10-28
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公开(公告)号: US20070100167A1公开(公告)日: 2007-05-03
- 发明人: Valerio Borzatta , Elisa Capparella , Carlotta Gobbi , Elisa Poluzzi
- 申请人: Valerio Borzatta , Elisa Capparella , Carlotta Gobbi , Elisa Poluzzi
- 优先权: ITMI2003A002103 20031030
- 国际申请: PCT/EP04/52710 WO 20041028
- 主分类号: C07C45/90
- IPC分类号: C07C45/90
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.
公开/授权文献
- US07402709B2 Process for synthesizing heliotropine and its derivatives 公开/授权日:2008-07-22
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