863239-59-2

Usage

Uses

Used in Pharmaceutical Industry:
(E/Z)-3α-hydroxy-6-ethylidene-7-keto-5β-cholan-24-oic acid Methyl ester is used as a reactant in the preparation of dual agonists of nuclear and membrane bile acid receptors. This application is significant because bile acid receptors play crucial roles in various physiological processes, including the regulation of cholesterol and glucose homeostasis, as well as the modulation of inflammation and energy metabolism. By acting as dual agonists, these compounds can potentially offer therapeutic benefits in treating a range of conditions, such as metabolic disorders, liver diseases, and inflammatory conditions.

Upstream product

• 863239-58-1 3α,7α-bis((trimethylsilyl)oxy)-6-ene-5β-cholanic acid methyl ester 
• 75-07-0 acetaldehyde 
• 67-56-1 methanol 
• 915038-24-3 (E/Z)-3α-hydroxy-6-ethylidene-7-keto-5β-cholan-24-oic acid 
• 77341-09-4 methyl 3α-(trimethylsilyloxy)-7-keto-5β-cholan-24-oate 
• 10538-59-7 7-ketolithocholic methyl ester 
• 52759-80-5 methyl 3α-7α-ditrimethylsilyloxy-5β-chol-6-en-24-oate 
• 4651-67-6 7-Ketolithocholic acid 
• 474-25-9 chenodeoxycholic acid 

Downstream Products

• 1537866-42-4 6α-ethyl-3α-formyloxy-7-keto-5β-cholan-24-oic acid 
• 1537866-43-5 6α-ethyl-3α-formyloxy-7-keto-24-nor-5β-cholan-23-nitrile 
• 1537866-44-6 6α-ethyl-3α-hydroxy-7-keto-24-nor-5β-cholan-23-oic acid 
• 1612191-83-9 3α,7α-dihydroxy-6α-ethyl-24-nor-5β-cholan-23-oic acid 
• 915038-25-4 3α-hydroxy-6β-ethyl-7-keto-5β-cholane-24-oic acid 
• 1000310-89-3 3α-tetrahydropyranyl hydroxy-6α-ethyl-7-keto-5β-cholan-24-oic acid 
• 1000310-91-7 3α-tetrahydropyranyloxy-6α-ethyl-7-keto-24-nor-5β-cholan-23-iodide 
• 1000310-93-9 3α-hydroxy-6α-ethyl-7-keto-24-nor-5β-cholan-23-iodide 
• 1000310-95-1 3α-tert-butyldimethylsilyloxy-6α-ethyl-7-keto-24-nor-5β-cholan-23-iodide 
• 1000310-97-3 3α-tert-butyldimethylsilyloxy-6α-ethyl-7-keto-24-nor-5β-cholan-23-ole 
• 1000310-99-5 3α-tert-butyldimethylsilyloxy-7α-hydroxy-6α-ethyl-24-nor-5β-cholan-23-ole 
• 1000311-02-3 3α-tert-butyldimethylsilyloxy-7α-hydroxy-6α-ethyl-24-nor-5β-cholan-23-sulphate triethylammonium salt 

Relevant academic research and scientific papers

Compound for treating metabolic diseases as well as preparation method and application thereof

The invention provides a compound for treating metabolic diseases, the compound has a structure represented by formula (I) or formula (II), or a racemate, a stereoisomer, a geometric isomer, a tautomer, a solvate, a hydrate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof. The compounds provided by the invention are FXR and/or TGR5 receptor activators, and the compounds havethe activity of activating FXR and/or TGR5 receptors, and can be used for preparing medicines for treating chronic liver diseases, metabolic diseases or portal hypertension.

Process Research and Impurity Control Strategy for Obeticholic Acid, a Farnesoid X Receptor Agonist

The process to obtain ICH-grade quality obeticholic acid (OCA) was improved, and the overall yield was 25.9%. The critical process parameters were established to reduce or avoid process-related impurities. The formation mechanisms, purge pathways, and control strategies for these impurities were also discussed for the first time. An high-performance liquid chromatography instrument utilizing the charged aerosol detection technique was applied for an impurity content assay in OCA for the first time. The developed process was robust and suitable for manufacturing scale-up.

PROCESS FOR THE PREPARATION OF 3α,7α-DIHYDROXY6α-ETHYL-5β-CHOLAN-24-OIC ACID

The present invention relates to an improved process for the preparation of 3α,7α-dihydroxy-6α-ethyl-5β-cholan-24-oic acid compound of formula-1, represented by the following structural formula: Formula-1 The present invention also relates to process for the preparation of ethylene diamine and tertiary butyl amine salts of 3α,7α-dihydroxy-6α-ethyl-5β-cholan-24-oic acid which are useful in the preparation of pure 3α,7α-dihydroxy-6α-ethyl-5β-cholan-24-oic acid.

New obeticholic acid preparation method

The invention relates to an obeticholic acid (represented by a structure formula 7) preparation method, which has characteristics of less purification steps, simple and convenient operation, high yield and low environmental pollution, and is suitable for industrial production. The formula 7 is defined in the specification.

STEROID DERIVATIVE FXR AGONIST

The present invention relates to a compound represented by formula (I), a tautomer thereof or a pharmaceutically acceptable salt thereof, and relates to applications thereof in the preparation of drugs for treating FXR related diseases.

Synthesis method of obeticholic acid and intermediate

The invention discloses a synthesis method of obeticholic acid and an intermediate. The method specifically comprises seven steps: an oxidation reaction, an esterification reaction, a protection reaction, an Aldol reaction, hydrogenation reduction, hydrolysis and a carbonyl reduction reaction with raw materials including chenodeoxycholic acid, NBS, concentrated sulfuric acid, methanol, sodium iodide, trimethyl silicon chloride, trimethylamine, acetaldehyde, boron trifluoride diethyl etherate, palladium on carbon, hydrogen, NaOH and NaBH4. The synthesis method of obeticholic acid and the intermediate is high in yield, low in cost, environmentally friendly, easy to operate and suitable for industrialization.

Sulfonylurea derivative and pharmaceutical composition and application thereof

The invention relates to a preparation method and application of a sulfonylurea compound and a composition containing the same component as FXR and / or TGR5 agonist, the FXR and / or TGR5 agonist is a compound shown as a formula (I), or a pharmaceutically acceptable salt, a solvate, a prodrug, an isomer and a stable isotope derivative thereof. The compounds can be used for treatment of FXR and / or TGR5 mediated diseases including primary biliary cirrhosis, nonalcoholic fatty liver, portal hypertension, bile acid diarrhea and cholestasis, type II diabetes and obesity and other field.

A high-purity aobeiAobei cholic acid preparation method (by machine translation)

The invention relates to a method for preparing high-purity aobeiAobei cholic acid. As shown in formula II compound chenodeoxycholic acid (CDCA) as the starting material, through oxidation, esterification, hydroxyl protection, ethylidene, catalytic hydrogenation, and carbonyl reduction of an ester of a reaction to obtain high-purity aobeiAobei cholic acid. The present invention provides a method of preparing aobeiAobei cholic acid with low toxicity, low pollution, high purity, stereoselectivity is good, there is little impurity content, mild reaction conditions, high safety, production simple operation and the like, and is suitable for industrial production. (by machine translation)

Process for preparing aobeiAobei cholic acid (by machine translation)

The invention application discloses a process for preparing aobeiAobei cholic acid, includes the following steps: AB - 1 — AB - 2 — AB - 3 — AB - 4 — AB - 5 — AB - 6 — AB - 7 — AB - 8 — AB - 9 — AB - 10, the preparation process in the process of preparing a simple and highly efficient reaction conditions, so as to ensure that the quality of the final product aobeiAobei cholic acid can be controlled. (by machine translation)

Preparation method for 3[alpha],7[alpha]-dihydroxyl-6[alpha]-ethyl cholanic acid

The invention belongs to the technical field of pharmaceutical synthesis, and discloses a preparation method for 3[alpha],7[alpha]-dihydroxyl-6[alpha]-ethyl cholanic acid. The method comprises the steps: with 3[alpha]-hydroxyl-7-carbonyl cholanic acid as a raw material, carrying out methyl esterification, and under alkaline and low temperature conditions and with estersil as a catalyst, carrying out a reaction with halogenated silane to obtain 3[alpha],7-di(trimethyl siloxy)-6-en-methyl cholanate; then under conditions of low temperature and boron trifluoride acetonitrile, carrying out a reaction with Mukaiyama aldol, to obtain 3[alpha]-hydroxyl-6-ethidene-7-carbonyl methyl cholanate; and then with palladium carbon as a catalyst, carrying out catalytic hydrogenation and deprotection reaction in an alkaline alcohol/aqueous solution, acidifying to obtain 3[alpha]-hydroxyl-6[alpha]-ethyl-7-carbonyl cholanic acid; and finally reducing with sodium borohydride to obtain the target product. The method has the advantages of simple synthesis process, mild conditions and high yield, and is suitable for industrialization.