- Preparation method of ursodesoxycholic acid
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The invention discloses a preparation method of ursodesoxycholic acid. Cholic acid is adopted as a raw material, and the ursodesoxycholic acid is prepared through 3 alpha-hydroxyl selective protection, 7 alpha-hydroxyl selective oxidation, ester group protection, 12 alpha-hydroxyl methanesulfonic acid esterification, 3 and 24 site protecting group selective hydrolysis, eliminating and catalytic hydrogenation. According to the preparation method, the low-cost cholic acid is adopted as the raw material, a synthesizing method is novel, low in cost, high in yield and mild in reaction condition, operation is easy and convenient, environmental friendliness is achieved, and industrial production is convenient.
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Paragraph 0114-0117
(2019/05/08)
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- Method for preparing obeticholic acid, ursodeoxycholic acid and 7-ketolithocholicacid
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The invention discloses a method for preparing obeticholic acid, 7-ketolithocholicacid and ursodeoxycholic acid. Cholic acid is used as a raw material for preparing obeticholic acid through selectiveprotection by a 3-alpha-hydroxyl group, selective oxidation of a 7-alpha-hydroxyl group, esterification of a 24th carboxyl group, methanesulfonation of a 12-alpha-hydroxyl group, elimination, hydrolysis, silylation, condensation, hydrolysis, catalytic hydrogenation, carbonyl reduction and other reactions; an intermediate is subjected to catalytic hydrogenation to prepare the 7-ketolithocholicacidand then is reduced to prepare the ursodeoxycholic acid. The method provided by the invention uses cheap cholic acid as the raw material, and has advantages of novel synthesis method, low cost, high yield, mild reaction condition, high simplicity in operation, environmental friendliness and high convenience in industrial production.
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Paragraph 0152-0155
(2018/11/03)
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- Method for synthesizing lithocholic acid from cholic acid
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The invention discloses a method for synthesizing lithocholic acid from cholic acid. According to the method, cholic acid is used as a starting raw material, and lithocholic acid is synthesized through the following four steps of reaction: selective protection of 3alpha-OH; oxidation of 7alpha-OH and 12alpha-OH into carbonyl groups; hydrolysis; and Huang Min-lon reduction. The raw material used in the method is easily available and cheap, and the method is few in synthesis steps and side reactions, simple in after-treatment, high in overall yield and suitable for industrial production.
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Paragraph 0048; 0049; 0050
(2017/09/01)
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- New biocompatible polyesters based on bile acids
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New biocompatible and biodegradable polyesters based on cholic acid or deoxycholic acid were synthesized by polycondensation reaction of 3-succinoyloxy-derivatives of bile acids with diethylene glycol. Chemical structure of the synthesized compounds has been proved by their elemental analysis, 1H-, 13C-NMR and IR spectra. Thermal behaviour and cristallinity of the polymers have been investigated.
- Stanciu, Magdalena Cristina,Nichifor, Marieta,Simionescu, Bogdan C.
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experimental part
p. 951 - 955
(2011/06/21)
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