Patent classifications
C07J53/00
NOVEL METHOD FOR SYNTHESIZING 25-OH CHOLESTEROL/CALCIFEDIOL FROM PHYTOSTEROL
The present invention discloses novel method for synthesizing vegan 25-OH cholesterol/Calcifediol from inexpensive crude phytosterol. According to the method, Phytosterols are reacted to form corresponding i-steroid through tosylation and methanolysis. i-steroid on reductive ozonolysis to C-22 alcohol and conversion via C-22 tosylate to C-22 iodide in good yield. Coupling of C-22 tosylate with Grignard reagent of 4-bromo-2-methyl-2-[(trimethylsilyl)oxy]butane followed by deprotection yielded 25-OH cholesterol. In a process variant, nickel mediated conjugate addition of C-22 iodide to an electron deficient alkene ethyl acrylate and treating corresponding ester with methyl magnesium bromide as means of installing the side chain of 25-OH cholesterol in high yield. Further bromination reaction of 25-OH cholesterol diacetate followed by dehydrobromination using TBAF yielded 25-OH 7-dehydrocholesterol. Further photo reaction of 25-OH 7-dehydrocholesterol in to previtamin D3 using high or medium pressure mercury lamp and subsequent thermal reaction of previtamin D3 to 25-OH vitamin D3 (Calcifediol) in good yield.
Method for Obtaining Gamma-Oryzanol
A method for obtaining γ-oryzanol comprises: (a) extracting an extract from a raw material containing γ-oryzanol by supercritical fluid extraction; (b) separating a pellet from the extract through solid-liquid separation; and (c) obtaining purified γ-oryzanol from the pellet.
Molecular host frameworks and methods of making and using same
Crystalline molecular framework:small molecule compounds. The molecular framework is formed from guanidinium cations and organosulfonate anions and the guanidinium cations and organosulfonate anions are associated via one or more hydrogen bond. The small molecule(s) is/are encapsulated by the molecular framework. Methods for making crystalline molecular framework:small molecule compounds may include combining guanidinium cations, organosulfonate anions, and small molecules in a single step. The crystalline molecular framework:small molecule compounds can be used to determine the structure of the small molecule(s).
METHOD FOR EXTRACTING ASTRAGALOSIDE IV FROM FRESH RADIX ASTRAGALI
The disclosure discloses a method for extracting Astragaloside IV from fresh Radix Astragali. The method comprises the following steps: cleaning and cutting fresh Radix Astragali roots into sections, and extracting with an ethanol solution for multiple times under an ultrasonic condition; merging the extracting solutions, concentrating to remove ethanol, hydrolyzing the concentrate with sodium hydroxide-calcium hydroxide mixed alkali, filtering the precipitate; then flocculating and precipitating by using a flocculating agent chitosan, and filtering; removing impurities through a flocculation-precipitation mode and filtering with a filter screen; separating through a macroporous adsorption resin, and finally purifying through recrystallization to obtain a high-purity Astragaloside IV. The method has the advantages of easily available raw materials, low cost, high Astragaloside IV extraction efficiency, high Astragaloside IV purity and simple process, the raw materials involved in the extraction process are non-toxic and harmless, and it is suitable for large-scale industrial production.
STEROID DERIVATIVE REGULATORS, METHOD FOR PREPARING THE SAME, AND USES THEREOF
Steroid derivative regulators, a method for preparing the same, and uses thereof are described. Specifically, a compound as shown in formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and uses thereof as a regulator of GABA A receptor for treating depression, convulsion, Parkinson's disease, and nervous system diseases are described, wherein the substituents of the formula (I) are as defined in the description.
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C-3 AND C-17 MODIFIED TRITERPENOIDS AS HIV-1 INHIBITORS
Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula I:
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These compounds are useful for the treatment of HIV and AIDS.
C-3 AND C-17 MODIFIED TRITERPENOIDS AS HIV-1 INHIBITORS
Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula I:
##STR00001##
These compounds are useful for the treatment of HIV and AIDS.
C-3 and C-17 modified triterpenoids as HIV-1 inhibitors
Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula I: ##STR00001##
These compounds are useful for the treatment of HIV and AIDS.
NEUROACTIVE STEROIDS AND COMPOSITIONS AND METHODS THEREOF
The invention provides novel neuroactive steroids and pharmaceutical compositions thereof, as well as methods of their preparation and use, in therapy of various diseases and conditions, for example, various neurological or brain diseases.
C17 POLAR-SUBSTITUTED HETEROAROMATIC SYNTHETIC TRITERPENOIDS AND METHODS OF USE THEREOF
Disclosed herein are compounds of the formula:
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wherein the variables are defined herein. Also provided are pharmaceutical compositions thereof. In some aspects, the compounds and compositions provided herein may be used as antioxidant inflammation modulators. In some aspects, the present disclosure provides methods wherein the compounds and composition described herein are used for the treatment of diseases and disorders, including those associated with inflammation and cancer.