10452-65-0Relevant articles and documents
METHOD FOR HOMOGENIZING BILE ACID DERIVATIVES
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, (2021/05/28)
The present invention relates to a process for producing bile acid derivatives having a protected hydroxyl group in the 3 position comprising contacting a bile acid derivative having an unprotected 3-alpha-hydroxyl group with a specific lipase. The present invention further relates to a bile acid derivative obtained or obtainable by the process, to the use of the bile acid derivative obtained or obtainable by the process for producing lithocholic acid and also to a process for producing lithocholic acid and to lithocholic obtained by the process. The invention further relates to the use of lithocholic acid obtained or obtainable by the process for producing ursodeoxycholic acid or ursodeoxycholic acid derivatives.
SYNTHETIC DERIVATIVES OF CHOLIC ACID 7-SULFATE AND USES THEREOF
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, (2020/07/05)
The compositions and methods provided herein are related, in part, to the discovery of cholic acid 7-sulfate as a treatment for diabetes. Provided herein is a method for treating a metabolic disorder (e.g., diabetes, obesity), or an inflammatory disease (e.g., Crohn's disease, inflammatory bowel disease, ulcerative colitis, pancreatitis, hepatitis, appendicitis, gastritis, diverticulitis, celiac disease, food intolerance, enteritis, ulcer, gastroesophageal reflux disease (GERD), psoriatic arthritis, psoriasis, and rheumatoid arthritis) in a subject in need thereof comprising administering to a subject a compound of Formulae (I)-(XVII).
Facial synthesis of key intermediate of obeticholic acid via Pd-catalyzed Kumada-Tamao-Corriu cross-coupling reaction
Di, Xiangjie,Han, Jie,Huang, Qingfei,Wang, Qiwei,Wang, Yuanhua,Wei, Xia,Zhong, Liu,Zhu, Jin,Zou, Sheng
, (2020/06/01)
Obeticholic acid (OCA) is used to treatment for Primary Biliary Cholangitis and other Famesoid X Receptor related diseases. Through the palladium catalyzed Kumada-Tamao-Corriu cross-coupling reaction, a novel and efficient method for synthesis of OCA with satisfied yield was successfully developed. The absolute configuration of the key intermediate was confirmed by Single-crystal X-ray Diffraction. It affords good strategy for large-scale synthesis of OCA.
Ketone-7- based cholic acid intermediate as well as preparation method and application thereof (by machine translation)
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, (2019/11/21)
The preparation method comprises the 7 - following steps: firstly, carrying out an esterification reaction on pig cholic acid as a starting raw material, and selectively protecting a leaving group 2,2 - through a special space 7 structure of the 6,7 pig cholic acid 3 6 7 - 7 - 7 7 6 α 6 6 7 7 . The method provided by the invention has 7 - the advantages of high purity, simple process flow and no special purification mode in the preparation process, and is suitable for industrial production. (by machine translation)
Preparation method of obeticholic acid and intermediate thereof
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Paragraph 2080; 0281, (2018/07/30)
The invention discloses a preparation method of obeticholic acid and an intermediate thereof. The invention provides a preparation method of a compound V. The preparation method of the compound V comprises the following steps: carrying out hydroxyl protective reaction on a compound VI and a hydroxyl protective reagent to obtain the compound V. The preparation method is simple and convenient to operate, low in cost, gentle in condition, environmentally friendly and suitable for industrialization.
Preparation method of obeticholic acid and intermediate thereof
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Paragraph 0297; 0298, (2018/07/30)
The invention discloses a preparation method of obeticholic acid and an intermediate thereof. The provided preparation method of the obeticholic acid comprises the following step: carrying out oxidizing reaction on a compound V and an oxidizing agent in an organic solvent to obtain a compound IV so as to obtain the final product. PG1 is a carboxyl protecting group, PG2 is a hydroxyl protecting group, and a component as shown in specification in the compound V and the compound IV independently shows that the ethidine is an E configuration, a Z configuration or a mixture of the E configuration and the Z configuration. The preparation method is simple and convenient to operate, low in cost, gentle in condition, environmentally friendly and suitable for industrialization.
Synthetic method of 7-keto-lithocholic acid
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Paragraph 0138; 0139, (2017/09/02)
The invention discloses a chemical synthetic method of an intermediate 7-keto-lithocholic acid (3alpha-hydroxyl-7-ketone-5beta-cholestane-24-acid) of obeticholic acid, and belongs to the field of organic chemical synthesis. According to the chemical synthetic method of the intermediate 7-keto-lithocholic acid (3alpha-hydroxyl-7-ketone-5beta-cholestane-24-acid) of obeticholic acid, cholic acid is adopted as a raw material, and through reactions of selective oxidization of 7alpha-hydroxyl, esterification of side chain carboxyl groups, esterification of 3alpha-hydroxyl, methanesulfonic acid esterification, elimination, hydrogenation, and hydrolysis of 12alpha-hydroxyl, the intermediate 7-keto-lithocholic acid (3alpha-hydroxyl-7-ketone-5beta-cholestane-24-acid) of obeticholic acid is synthesized. According to the chemical synthetic method of the intermediate 7-keto-lithocholic acid (3alpha-hydroxyl-7-ketone-5beta-cholestane-24-acid) of obeticholic acid, cheap cholic acid is adopted as the raw material, the synthesis method is novel, low in cost, high in yield and environmentally friendly, which facilitates industrialized production.
PROCESS FOR PREPARATION OF OBETICHOLIC ACID
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, (2018/01/17)
The invention of the present application relates to the process for the preparation of intermediates of obeticholic acid and their conversion to obeticholic acid. The process involves the conversion of compound of formula (VI) to compound of formula (VII) in presence of an organic base.
Chenodeoxycholic acid compound and preparation method and application thereof
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, (2016/10/07)
The invention discloses a compound with a structural formula (I) and a pharmaceutically-acceptable salt, solvate or amino acid conjugate thereof (shown in the description). Six substituent groups are respectively located at alpha or beta positions, the R1 represents COOH or OSO3H, and the R2 represents a halogen alkyl group, a naphthenic base, a naphthenic-alkyl group, a heterocyclic group, a heterocyclic-alkyl group, a heterocyclic aryl group, a heterocyclic aryl-alkyl group, an acyl group or an alkoxyalkyl group.
A Facile Route to Ursodeoxycholic Acid Based on Stereocontrolled Conversion and Aggregation Behavior Research
Dou, Qian,Jiang, Zhongliang
, p. 588 - 594 (2016/02/14)
A facile route to ursodeoxycholic acid (UDCA) and its aggregation behavior in aqueous phase solution, which is rarely known, are reported. The starting material, hyodeoxycholic acid (HDCA), is a relatively less expensive material and more easily obtained compared with chenodeoxycholic acid (CDCA). A facile route was developed to synthesize UDCA from HDCA with a Shapiro reaction as the key step and in 26% overall yield. A new strategy using organosilane reagent considering its stability, nontoxicity, and abundance in nature was carried out for a more rapid route and higher yield. It was found that the critical micelle concentration value, which is a critical value for surfactants of bile salts, was influenced by the number of hydroxyl groups.
