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NOVEL PROCESS FOR THE PREPARATION OF VORINOSTAT
专利权人:
GENERICS [UK] LIMITED
发明人:
GAITONDE, ABHAY,CHOUDHARI, BHARATI
申请号:
NZ58695509
公开号:
NZ586955A
申请日:
2009.02.06
申请国别(地区):
NZ
年份:
2012
代理人:
摘要:
Disclosed is a process for the preparation of vorinostat, comprising the following steps: (a) reaction of suberic acid with a haloformate such as methyl chloroformate in the presence of a base such as triethylamine (thereby resulting in an insoluble precipitate of triethylammonium chloride which can be removed by filtration) (b) reaction of aniline with the product of step (a) (c) reaction of a haloformate with the product of step (b) in the presence of a base (i.e. another equivalent of methyl chloroformate / triethylamine) (d) reaction of hydroxylamine with the product of step (c) and (e) isolation of the product vorinostat wherein the reaction is desirably conducted in an organic solvent selected from the group comprising dimethyl sulfoxide, tetrahydrofuran, acetonitrile, dimethylformamide or dimethyl acetamide and wherein steps (a)-(d) can be conducted sequentially without isolation of the corresponding intermediates (i.e. in a one pot synthesis). Also disclosed is high purity vorinostat obtained by the above process. Suitable uses of vorinostat are also disclosed. .
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