34results about "Ketal steroids" patented technology

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.

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.

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.

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.

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.

The invention belongs to the technical field of chemical synthesis, and particularly relates to a preparation method of methylprednisolone and an intermediate compound thereof. The preparation method comprises the following steps: by taking cortisone as a raw material, carrying out 17 and 21 site upper protecting groups and 3 site upper protecting groups, and carrying out reduction, so as to obtain a methylprednisolone intermediate compound shown as a formula V; and carrying out 5 and 6-site epoxidation, Grignard reaction, 3-site protecting group removal, 4 and 5-site dehydration elimination, 1 and 2-site dehydrogenation and 17 and 21-site protecting group removal on the compound in the formula V to obtain methylprednisolone. The structural formula of the compound of formula V is shown in the specification. The preparation process has the advantages of high yield, high purity, low cost, simplicity in operation and suitability for industrial production.

The invention discloses a Pinellinoic acid derivative shown in a general formula (I) (the specific substituent definition is shown in the specification), a pharmaceutical composition with the Pinellinoic acid derivative as an active component, a preparation method of the compound and application of the Pinellinoic acid derivative in preparation of drugs for inhibiting cholesterol synthesis activity and drugs for treating non-alcoholic fatty liver diseases. Belongs to the technical field of medicines. Pharmacological test results indicate that the Songlinolenic acid derivative has good sterol ester de novo synthesis and fatty acid de novo synthesis inhibitory activity. The compound can be used as a novel high-efficiency sterol lipid synthesis inhibitor, can be used for treating diseases related to sterol lipid metabolism, and has a good application prospect.

To provide 3α-hydroxy-17β-amide neuroactive steroids and compositions thereof.SOLUTION: Provided herein is a compound of the formula (I) in the figure or pharmaceutically acceptable salt thereof, where R2a, R2b, R4a, R4b, R6, R7, R11a, R11b, R16, R17, R3, R5, R19, RX and RY are as defined herein. Also provided herein are pharmaceutical compositions comprising a compound of the formula (I) and methods of using the compounds, e.g., in treatment of CNS-related disorders. Provided herein are compounds designed, for example, to act as GABA modulators. In some embodiments, such compounds are expected to be useful as therapeutic agents for treating a CNS-related disorder.SELECTED DRAWING: None

Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein ------, R1, R2, R5, A and L are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e.g., such for inducing sedation and / or anesthesia.

A method for preparing a key intermediate 7K of ursodeoxycholic acid (UDCA). The key intermediate 7K of UDCA is prepared from BA by means of eight steps of reaction below: first subjecting the raw material BA to sulfonylation and then to alkylation with a malonic diester so as to construct a 21-position side chain, in which steps, sulfonylation and alkylation proceed readily, the conditions are mild, and there are few by-products and impurities; and then subjecting same to ketal protection, oxidation, hydrolysis, hydrogenation, hydrolysis and decarboxylation.

The present application provides an intermediate compound and a preparation method therefor and an application thereof. The intermediate compound has the following structural formula (I). By using the intermediate compound of the present application, dedrogesterone can be conveniently synthesized only by performing AB ring double bond construction and side chain modification, the total yield is high, and the route is short.

The invention belongs to the technical field of organic photochemical synthesis, and particularly relates to a method for synthesizing 9 beta, 10 alpha-dehydroprogesterone ketal. According to the method, a narrow-linewidth light source with an adjustable central wavelength range and an emission spectrum half-peak width of not more than 5 nanometers is used for the first time to realize one-pot two-step photochemical synthesis of 9beta, 10alpha-dehydroprogesterone ketal; according to the method, the quasi-quantitative photochemical reaction from the raw material 9 [alpha], 10 [beta]-dehydroprogesterone ketal to the target product 9 [beta], 10 [alpha]-dehydroprogesterone ketal can be realized. After the 9alpha, 10beta-dehydroprogesterone ketal is subjected to a one-pot two-step photochemical reaction, the total amount of byproducts does not exceed 3wt% according to the input amount of the 9alpha, 10beta-dehydroprogesterone ketal; the yield of the 9beta, 10alpha-dehydroprogesterone ketal is up to 96.7% on the basis of consumed 9beta, 10beta-dehydroprogesterone ketal, and the yield of the target product 9beta, 10alpha-dehydroprogesterone ketal is more than two times that of the existing method for preparing the 9beta, 10alpha-dehydroprogesterone ketal.

The present invention provides a synthesis method for a 7-ketolithocholic acid or an intermediate thereof, which is prepared from a new intermediate I-1. According to the method, phytosterol degradation product bisnoralcohol is used as a starting material, and the 7-ketolithocholic acid or the intermediate thereof is obtained by means of an oxidation reaction, a Knoevenagel reaction (or wittig reaction), hydrogenation, a ketal protection reaction, an allylic oxidation reaction, ketal removal protection, and the hydrogenation. According to the method of the present invention, raw materials are easily available, the yield is high, reaction conditions are simple and mild, and the method is suitable for industrial production.