Process for the preparation of S-fluoromethyl-6,9-difluoro-11-hydroxy-16-methyl-17-propionyloxy-3-oxo-androsta-1, 4-diene-17-carbothioate and intermediates

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专利权人:

Generics [UK] Limited

发明人:

Pokharkar, K.,Gore, Vinayak G.,Wakchure, V.,Gadakar, Mahesh

申请号：

AU2013202843

公开号：

AU2013202843B2

申请日:

2013.04.08

申请国别(地区):

AU

年份:

2015

代理人:

摘要：

#$%^&*AU2013202843B220151112.pdf#####PROCESS FOR THE PREPARATION OF S-FLUOROMETHYL-6,9DIFLUORO-1 1-HYDROXY-16-METHYL-17-PROPIONYLOXY-3-OXOANDROSTA-1,4-DIENE-17-CARBOTHIOATE AND INTERMEDIATES ABSTRACT The present invention relates to a process for the preparation of steroidal 17p-carboxylic thioates. More particularly the present invention relates to a convenient and efficient synthesis of steroidal 17p-carboxylic thioates, such as fluticasone propionate formula (I), using soluble mixed fluorides to introduce fluorine by displacing an appropriate leaving group X in compounds formula (II) resulting in selective and controlled fluorination. The present invention also relates to intermediates formula (II) and their preparation.

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