发明名称 Process for synthesizing heliotropine and its derivatives
摘要 A new high-yield, easily industrialized process for synthesizing compounds of formula (IV), in which X<SUB>1 </SUB>and X<SUB>2</SUB>, 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<SUB>1</SUB>)n and (OX<SUB>2</SUB>)m taken together form an O-T-O group where T is chosen from -CH<SUB>2</SUB>-, -CH<SUB>2</SUB>CH<SUB>2</SUB>, -CH<SUB>2</SUB>CH<SUB>2</SUB>CH<SUB>2</SUB>-, -C(CH<SUB>3</SUB>)<SUB>2</SUB>-. 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.
申请公布号 US7402709(B2) 申请公布日期 2008.07.22
申请号 US20040577846 申请日期 2004.10.28
申请人 ENDURA S.P.A. 发明人 BORZATTA VALERIO;CAPPARELLA ELISA;GOBBI CARLOTTA;POLUZZI ELISA
分类号 C07C45/90;C07D317/54 主分类号 C07C45/90
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