79results about "Ketal steroids" patented technology

The invention discloses a synthesis method of an unsaturated ketone or arone compound, which comprises the following steps: at a certain temperature, taking unsaturated hydrocarbon or aromatic hydrocarbon as a raw material, taking an N-hydroxyimide compound as a catalyst, adding an organic solvent for dissolving, introducing oxygen or air into a reaction solution under the irradiation of visible light, and carrying out oxidation reaction to obtain the unsaturated ketone or arone compound. And carrying out post-treatment separation to obtain the unsaturated ketone or arone. According to the method, air, oxygen-enriched gas or oxygen is used as a harmless oxidizing agent, visible light is used as an energy source to promote the reaction, and the method has the advantages that the reaction process is green and efficient, the cost is low, the dosage of the catalyst is small, and most of the catalyst can be recycled and reused; the atom economy is high.

Provided herein are compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein n, R 19 , R 5 , R 3a , R 6a , R 6b , R 1 , R 2a , R 2b , R 4a , R 4b , R 7a , R 7b , R 11a , R 11b , R 12a , R 12b , R 17b , R 15a , R 15b , R 16a and R 16b is defined herein. Also provided herein are pharmaceutical compositions comprising compounds of formula (I) and methods of using such compounds, for example, in the treatment of CNS-related disorders. JPEG2022504607000068.jpg4662(I)

The present invention discloses a synthesis method of ursodeoxycholic acid by using the plant-derived compound BA as a raw material to synthesize ursodeoxycholic acid through the steps of ethylene glycol or neopentyl glycol protection, oxidation, Wittig reaction, deprotection, reduction and hydrolysis, etc. The raw materials used for the synthesis of ursodeoxycholic acid in the present invention are cheap and easy to get, the synthesis steps are easy to operate, the yield is high, the reaction is environmentally friendly, and the industrial production is convenient.

Disclosed herein are deuterated compounds and transition metal catalyzed methods for making deuterated compounds. The disclosed methods are regioselective and enantioselective and may be utilized to prepare isomerically and / or enantiomerically pure or enriched deuterated compounds. The disclosed methods also may be modified in order to prepared fluorinated compounds.

As used herein, a compound of formula (1-I): JPEG2022538300000478.jpg47165, or a pharmaceutically acceptable salt thereof, wherein R 2a , R 2b , R 3 , R 4a , R 4b , R 5 , R 6a , R 6b , R 11a , R 11b , R 16a , R 16b , R 19 , R 18 , X, q, r, s, t, u, and n are defined herein. Also provided herein are pharmaceutical compositions comprising the compounds of formula (1-I), and methods of using the compounds, e.g., in the treatment of CNS-related disorders.

Described herein are steroids of Formula (I):and pharmaceutically acceptable salts thereof, wherein R1, R2a, R2b, R3, R4, R5a, R5b, R6, and Z are as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and / or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and / or withdrawal syndromes, and tinnitus.

The present invention relates to compounds which are active against parasitic infections, such as protozoan parasite infections (including flagellate parasite infections, ciliate parasite infections, amoeba parasite infections and apicomplexan parasite infections) and helminth infections. The present invention also relates to compositions comprising the compounds, and methods of treating or preventing parasitic infections, such as protozoan parasite infections (including flagellate parasite infections, ciliate parasite infections, amoeba parasite infections and apicomplexan parasite infections) and helminth infections, using the compounds.

To provide compositions and methods for treating CNS disorders.SOLUTION: Provided herein are compounds of Formula (I-X) in the figure or a pharmaceutically acceptable salt thereof. Also provided are pharmaceutical compositions comprising the compounds, and methods of using the compounds, e.g., in treatment of CNS-related disorders. Provided herein are compounds designed, e.g., to act as GABAA receptor modulators. In some embodiments, such compounds are envisioned to be useful as therapeutic agents for treating a CNS-related disorder (e.g., a disorder described herein, such as postpartum depression or major depressive disorder).SELECTED DRAWING: None

The invention provides a preparation method of 17 alpha-hydroxypregna-4-ene-3, 11, 20-triketone and an intermediate compound prepared by the preparation method, and relates to the technical field of medicine synthesis. The target product disclosed by the invention is prepared by taking 11 alpha-hydroxy-4-androstenedione as a starting material and carrying out six-step reaction, namely oxidation, ethynylation, ketalation, sulfonylation, etherification and hydrolysis. The starting material 11 alpha-hydroxy-4-androstenedione of the process is prepared from 4-androstenedione through enzyme transfer, and compared with 11 alpha, 17 alpha-dihydroxyprogesterone prepared from 17 alpha-hydroxyprogesterone through enzyme transfer, the enzyme transfer technology of the former is more mature, the conversion rate and the yield are higher, and the cost is lower. Meanwhile, the preparation method disclosed by the invention is easy to operate and implement in production and high in reaction conversion rate, avoids the use of a highly toxic reagent acetone cyanohydrin, and is more beneficial to large-scale industrial production.

The invention provides indole C3-O functionalized derivatives as well as a preparation method and insecticidal and antibacterial application thereof, and relates to the technical field of pesticide development. The indole C3-O functionalized derivative provided by the invention has a structure of a general formula (1), is prepared through a free radical cyclization reaction catalyzed by N-heterocyclic carbene (NHC), does not need a transition metal catalyst, and efficiently constructs a C3-site oxygen functional group by taking o-nitroalkyne or cis-o-nitrostyrene and aldehyde as raw materials through multi-step series conversion in an inert atmosphere. The method has the advantages of being high in atom economy, good in functional group compatibility, easy and convenient to operate, environmentally friendly and the like. The obtained derivative shows remarkable activity in prevention and treatment of various agricultural diseases and insect pests such as rice sheath blight disease, aflatoxin and brown planthopper, can be prepared into various pesticide preparations, has the characteristics of broad spectrum, high efficiency and low toxicity, and is suitable for development of green pesticides.

The present invention discloses a short, cost effective process for preparation of cholesterol from bisnoralcohol (BA).

The present invention provides a method for synthesizing 7-ketolithocholic acid or its intermediates produced from a novel intermediate I-1. In the method, bisnoralcohol, a decomposition product of phytosterol, is used as a starting material, and 7-ketolithocholic acid or its intermediates can be obtained through oxidation, Knoevenagel reaction (or Wittig reaction), hydrogenation, esterification, ketal protection, allylic oxidation, ketal deprotection, and hydrogenation. The method of the present invention allows easy availability of raw materials, high yields, simple and mild reaction conditions, and is suitable for industrial production.

Provided in the present invention is a method for synthesizing a 7-ketolithocholic acid intermediate, the method comprising preparing compound OB-1 in an amide solvent to obtain a 7-ketolithocholic acid intermediate OB. The method of the present invention has the advantages of readily available of raw materials, a high yield, simple and mild reaction conditions, and suitability for industrial production.

Compounds and compositions for the activation of SERCA2a are disclosed. In particular, provided are compounds that act as predominantly pure or pure SERCA2a activators while only moderately inhibiting the Na+ / K+ ATPase. In general, the disclosed compounds are derivatives of androstane having the formula (I). Also disclosed herein are pharmaceutical compositions comprising one or more of the compounds of formula (I) for use for the treatment of heart failure.

The present invention provides a method for synthesizing 7-ketolithocholic acid or its intermediates produced from a novel intermediate I-1. In the method, bisnoralcohol, a decomposition product of phytosterol, is used as a starting material, and 7-ketolithocholic acid or its intermediates can be obtained through oxidation, Knoevenagel reaction (or Wittig reaction), hydrogenation, esterification, ketal protection, allylic oxidation, ketal deprotection, and hydrogenation. The method of the present invention allows easy availability of raw materials, high yields, simple and mild reaction conditions, and is suitable for industrial production.

Compounds and compositions for the activation of SERCA2a are disclosed. In particular, provided are compounds that act as predominantly pure or pure SERCA2a activators while only moderately inhibiting the Na+ / K+ ATPase. In general, the disclosed compounds are derivatives of androstane having the formula (I)Also disclosed herein are pharmaceutical compositions comprising one or more of the compounds of formula (I) for use for the treatment of heart failure.

(3α, 3β) disubstituted 17β steroid compounds, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof are provided for the prevention and treatment of various CNS-related conditions. [Solution] In yet another aspect, a method is provided for treating or preventing a CNS-related condition associated with NMDA modulation, comprising administering to a subject in need thereof an effective amount of a compound or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition thereof.

The invention discloses a method for preparing 3 beta-hydroxy-androstane-5-ene-17-ketone-D6 (abbreviated as dehydroepiandrostene-D6) from androstane-4-ene-3, 17-diketone-D8 (abbreviated as androstenediketone-D8), and the dehydroepiandrostene-D6 is prepared from the androstenediketone-D8 as a raw material through five steps of enol esterification, upper protection, reduction, deprotection and deuterium hydrogen replacement. According to the preparation method, androstenedione-D8 is taken as a raw material, enol esterification is firstly carried out, then 17-carbonyl is subjected to ethylene glycol protection, 3-carbonyl is reduced through sodium borodeuteride under the condition of a deuterated solvent, deuterium atoms are introduced to the 3-position and the 4-position respectively, then ethylene glycol protection is removed, finally deuterium hydrogen replacement is carried out, the deuterium atom at the 16-position is replaced with a hydrogen atom, and the androstenedione-D8 is obtained. And the dehydroepiandrosterone D6 is prepared and obtained. The method disclosed by the invention is mild in reaction condition and simple to operate, can realize efficient preparation of dehydroepiandrosterone D6, and has an important application prospect.

The present invention discloses a short, cost effective process for preparation of cholesterol from bisnoralcohol (BA).

The invention relates to the technical field of medicine synthesis, and particularly discloses application of filtering liquid in photocatalytic preparation of a key intermediate of didrogesterone. The invention provides an application of a filtering solution in photocatalytic preparation of a key intermediate of didrogesterone. The filtering solution comprises a soluble copper salt, a soluble manganese salt and a soluble chromium salt as an aqueous solution of solutes, the key intermediate of the didrogesterone is 9beta, 10alpha-pregna-4, 6-diene-3, 20-diethylene glycol ketal. The filter liquid provided by the invention is applied to a reaction for preparing the key intermediate of the didrogesterone through photocatalysis, the yield of the key intermediate of the didrogesterone can be remarkably increased, the purity can reach 80.2%, the yield can reach 91.1%, and compared with a traditional filter sheet form, the production investment is lower, and large-scale industrial production of the key intermediate of the didrogesterone can be realized.

The present invention belongs to the technical field of organic synthesis, and relates to a method for preparing a geminal bis(boryl)cyclopropane compound. The present invention forms a γ-iodine-substituted geminal di(boryl) ester compound intermediate by an intermolecular halogen atom transfer radical addition reaction, and then the γ-iodine-substituted geminal di(boryl) ester compound intermediate is deprotonated and alkylated in the presence of a base to produce a cyclization product, a geminal bis(boryl)cyclopropane compound. The method provided by the present invention can synthesize a geminal bis(boryl)cyclopropane compound by a one-pot method from an olefin combined with (diborylmethyl) iodide under visible light irradiation, is simple to operate, and provides a rapid way to synthesize highly functionalized compound molecules.

The invention discloses a method for preparing testosterone D3 by using 17-carbonyl androstane-5-ene-3-ethylene ketone-16 and 16-D2, which is characterized in that the 17-carbonyl androstane-5-ene-3-ethylene ketone-16 and 16-D2 is used as a raw material, and the testosterone D3 is prepared by two steps of reduction and deprotection. According to the preparation method, 17-carbonyl androstane-5-ene-3-ethylene ketone-16, 16-D2 is taken as a raw material, reduction is carried out through sodium boron deuteride, deuterium atoms are introduced to the 17 site, then deprotection is carried out, and high-abundance testosterone D3 (abundance gt; 96%). The invention also provides a novel compound of formula (2). The raw materials are easy to prepare, the deuteration efficiency is high, the reaction condition is mild, the operation is simple, the efficient preparation of testosterone D3 can be realized, and the testosterone D3 has a wide application prospect.

The present invention provides a method for synthesizing 7-ketolithocholic acid intermediate, which comprises the step of obtaining 7-ketolithocholic acid intermediate OB from compound OB-1 in an amide solvent. The method of the present invention has easy availability of raw materials, high yield, simple and mild reaction conditions, and is suitable for industrial production.

The present disclosure is generally directed to neuroactive 19-alkoxy-17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and / or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.