Title:
PROCESS FOR PREPARING OBETICHOLIC ACID
Document Type and Number:
WIPO Patent Application WO/2020/119836
Kind Code:
A8
Abstract:
A process for preparing obeticholic acid, wherein the 7-keto-litocholic acid amide of formula (II), where R1, R2 are a C1-C6 n-alkyl, or together a C5-C6 cycle and the protecting group on the hydroxyl in position 3 is a carbamoyl with the same substitution as the amide, is converted to the 7-trimethylsilyl enol ether of formula (III), which is then converted by reaction with an alkylation agent to the 6-ethylidene-derivative of formula (IV), which is hydrogenated to the compound of formula (V) and then simultaneously deprotected in position 3 and hydrolysed to the compound of formula (VI) and then reduced to obeticholic acid of formula (VII).
Inventors:
STOHANDL JIRI (CZ)
FRANTISEK JAROSLAV (CZ)
HRBACOVA SANDRA (CZ)
SOVA PETR (CZ)
KALA MATEJ (CZ)
FRANTISEK JAROSLAV (CZ)
HRBACOVA SANDRA (CZ)
SOVA PETR (CZ)
KALA MATEJ (CZ)
Application Number:
PCT/CZ2019/000009
Publication Date:
July 23, 2020
Filing Date:
February 12, 2019
Export Citation:
Assignee:
FARMAK A S (CZ)
International Classes:
C07J9/00; C07J41/00; C07J51/00
Attorney, Agent or Firm:
JIROTKOVA, Ivana et al. (CZ)
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