105660-11-5Relevant articles and documents
Bile acids: Lipase-catalyzed synthesis of new hyodeoxycholic acid derivatives
Chanquia, Santiago N.,Ripani, Erika,Baldessari, Alicia,García Li?ares, Guadalupe
, p. 45 - 51 (2018)
In this work we present an efficient, environmentally friendly approach to the synthesis of a series of hyodeoxycholic acid derivatives applying Biocatalysis. Fifteen acetyl and ester derivatives, twelve of them new, were obtained through an enzymatic strategy in a fully regioselective way and in very good to excellent yield. In order to find the optimal reaction conditions, the influence of several parameters such as enzyme source, alcohol or acylating agent:substrate ratio, enzyme:substrate ratio, temperature and reaction solvent was considered. The excellent results obtained made this procedure very efficient, particularly considering the low amount of enzyme required. In addition, this methodology uses mild reaction conditions and has reduced environmental impact, making biocatalysis a suitable way to obtaining these bile acids derivatives.
Method for preparing ursodeoxycholic acid
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Paragraph 0059; 0060, (2017/07/20)
The invention belongs to the field of medicine, and particularly relates to a method for preparing an ursodeoxycholic acid. The method comprises the following steps: performing esterification reaction to obtain a compound shown in formula II by taking an HDCA (hyodeoxycholic acid) as a starting raw material; performing selective hydroxy protection reaction to obtain a compound shown in formula III; performing hydroxy protection reaction to obtain a compound shown in formula IV; performing elimination reaction to obtain a compound shown in formula V; performing oxidation reaction on the compound shown in formula V under the action of tert-butyl hydroperoxide and pyridinium chlorochromate to obtain a compound shown in formula VI; performing hydrolysis to obtain a compound shown in formula VII; performing reduction to obtain the ursodeoxycholic acid shown in formula I. According to the method, the ursodeoxycholic acid is prepared by taking the HDCA as the starting raw material, so that not only can the problem of raw material shortage be solved, but also the method is convenient to operate, low in byproduct rate and cost, mild in reaction condition and suitable for large-scale production of the ursodeoxycholic acid.
