17results about "Ketal steroids" patented technology

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.

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 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.

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

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.

This invention provides a method for synthesizing 7-ketolithocholic acid or its intermediates, which is prepared via a novel intermediate I-1. The method uses phytosterol degradation product dichlorol as a starting material and proceeds through oxidation, Knoevenagel reaction (or Wittig reaction), hydrogenation, esterification, ketal protection, allylic oxidation, deketal protection, and hydrogenation to obtain 7-ketolithocholic acid or its intermediates. The method of this invention uses readily available raw materials, has high yield, and employs simple and mild reaction conditions, making it suitable for industrial production.