MORIARTY, ROBERT M.,DAVID, NATHANIEL E.,MAHMOOD, NADIR AHMEDUDDIN,PRASAD, ACHAMPETA RATHAN,SWARINGEN, ROY A.,REID, JOHN GREGORY,SAHOO, AKHILA KUMAR
申请号：
ES11181831
公开号：
ES2550504T3
申请日:
2008.06.18
申请国别(地区):
ES
年份:
2015
代理人:
摘要：
A method for preparing deoxycholic acid (DCA) or a pharmaceutically acceptable salt thereof: ** Formula ** comprising said method (a) reacting 9α-hydroxyandrost-4-in-3,17-dione 1 with H2 under conditions of hydrogenation to form compound 2 ** Formula ** (b) react compound 2 with acid to form compound 3 ** Formula ** (c) react compound 3 with a reducing agent to form compound 4 as a mixture of 4 and 5 ** Formula ** (d) react compound 4 with a two-carbon olefination reagent under olefin formation conditions to form compound 6 ** Formula ** (e) convert compound 6 in a compound of the formula 7 ** Formula ** (f) reacting the compound of the formula 7 with an alkyl propriolate of the formula CH-CC (O) OR or an alkyl acrylate of the formula CH2>； = CHC (O) OR in which R is alkyl, in the presence of a Lewis acid to form a compound of the formula 8 wherein P is a protective group, R is alkyl and the dashed line ------ is a single or double bond； ** Formula ** (g) react the compound of formula 8 with H2 under hydrogenation conditions to form a compound of the formula 9 in which P is a protecting group and R is alkyl； ** Formula ** (h) reacting the compound of the formula 9 with an oxidizing agent to form a compound of the formula 10 wherein P is a protecting group such as acetyl and R is alkyl； ** Formula ** (i) reacting the compound of formula 10 with H2 under hydrogenation conditions to form a compound of formula 11 in where P is a protecting group and R is alkyl； ** Formula ** (j) reacting the compound of formula 11 with a reducing agent to form a compound of formula 12 in which P is a protecting group and R is alkyl； ** Formula ** (k) exposing the compound of formula 12 to deprotection conditions to form a compound r thereof and at suitable hydrolysis conditions to form deoxycholic acid or a pharmaceutically acceptable salt thereof.Un método para preparar ácido desoxicólico (DCA) o una sal farmacéuticamente aceptable del mismo:**Fórmula** comprendiendo dicho método (a)
