The present disclosure relates to a synthesis method for halofuginone and its intermediates, with the reaction formulas as shown below, wherein, R.sub.1 is selected from: methyl, ethyl, propyl, isopropyl or tert-butyl:, R.sub.2 is selected from: methyl, ethyl:, R.sub.3 is selected from: methoxyformyl, ethoxyformyl, tert-butoxyformyl, benzyloxyformyl, trichloroethoxyformyl or benzyl. The synthesis method in the present disclosure has many advantages, such as simple process, low cost, few by-products in the synthesis process, simple purification process, no need for column chromatography purification, high product yield, few impurities, high purity, controllable product quality, easy to meet the requirements of ICH declaration, and it can be used for industrial production of halofuginone.

##STR00001##

A nonionic Gemini surfactant, (octylphenol polyoxyethylene ether disubstituted) dicarboxylic acid diphenyl ether has a structural formula of: ##STR00001##
and is prepared by a two-step reaction: S1, diphenyl ether 4,4′-dicarboxylic acid is subjected to an acyl chlorination reaction to obtain diphenyl ether 4,4′-dicarbonyl dichloride; S2, diphenyl ether 4,4′-dicarbonyl dichloride is subjected to an esterification reaction with octylphenol polyoxyethylene ether (OP-10) to obtain the target product (octylphenol polyoxyethylene ether disubstituted) dicarboxylic acid diphenyl ether. The surfactant is expected to be applied in tertiary oil recovery as an alkali/surfactant, in polymer/surfactant binary composite flooding, in alkali/surfactant/polymer ternary composite flooding, as a microemulsion emulsifier and the like, and it can also be compounded with a common surfactant to reduce the use cost, and thus create conditions for its large-scale application.

A nonionic Gemini surfactant, (octylphenol polyoxyethylene ether disubstituted) dicarboxylic acid diphenyl ether has a structural formula of: ##STR00001##
and is prepared by a two-step reaction: S1, diphenyl ether 4,4′-dicarboxylic acid is subjected to an acyl chlorination reaction to obtain diphenyl ether 4,4′-dicarbonyl dichloride; S2, diphenyl ether 4,4′-dicarbonyl dichloride is subjected to an esterification reaction with octylphenol polyoxyethylene ether (OP-10) to obtain the target product (octylphenol polyoxyethylene ether disubstituted) dicarboxylic acid diphenyl ether. The surfactant is expected to be applied in tertiary oil recovery as an alkali/surfactant, in polymer/surfactant binary composite flooding, in alkali/surfactant/polymer ternary composite flooding, as a microemulsion emulsifier and the like, and it can also be compounded with a common surfactant to reduce the use cost, and thus create conditions for its large-scale application.

Methods are provided for modulating MRGPR X4 generally, or for treating a MRGPR X4 dependent condition more specifically, by contacting the MRGPR X4 or administering to a subject in need thereof, respectively, an effective amount of a compound having the structure of Formula (I):

##STR00001##

or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein n, x, A, Q.sub.1, Q.sub.2, Z, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are as defined herein. Pharmaceutical compositions containing such compounds, as well as to compounds themselves, are also provided.

The present invention provides a process for purifying a monoterpene or sesquiterpene having a purity greater than about 98.5% (w/w). The process comprises the steps of derivatizing the monoterpene (or sesquiterpene) to produce a monoterpene (or sesquiterpene) derivative, separating the monoterpene (or sesquiterpene) derivative, and releasing the monoterpene (or sesquiterpene) from the derivative. Also encompassed by the scope of the present invention is a pharmaceutical composition comprising a monoterpene (or sesquiterpene) having a purity greater than about 98.5% (w/w). The purified monoterpene can be used to treat a disease such as cancer. The present monoterpene (or sesquiterpene) may be administered alone, or may be co-administered with radiation or other therapeutic agents, such as chemotherapeutic agents.

The present invention provides a process for purifying a monoterpene or sesquiterpene having a purity greater than about 98.5% (w/w). The process comprises the steps of derivatizing the monoterpene (or sesquiterpene) to produce a monoterpene (or sesquiterpene) derivative, separating the monoterpene (or sesquiterpene) derivative, and releasing the monoterpene (or sesquiterpene) from the derivative. Also encompassed by the scope of the present invention is a pharmaceutical composition comprising a monoterpene (or sesquiterpene) having a purity greater than about 98.5% (w/w). The purified monoterpene can be used to treat a disease such as cancer. The present monoterpene (or sesquiterpene) may be administered alone, or may be co-administered with radiation or other therapeutic agents, such as chemotherapeutic agents.

Provided are a novel compound exhibiting the effect of treating, preventing or ameliorating lymphedema, and a composition including the same as an active ingredient, and may be applied as a medicament product, functional food or food supplement, or cosmetics. The compound used as an active ingredient compound according to the disclosure exhibits a remarkable ameliorating effect on lymphedema in various aspects such as TNFα production inhibitory activity, metabolic stability, solubility, and blood exposure.

The present invention relates to monoterpenoid and phenylpropanoid containing derivative compounds, methods of making the compounds, compositions comprising the compounds, and methods of repelling pests using the compounds and/or compositions.

The present invention relates to monoterpenoid and phenylpropanoid containing derivative compounds, methods of making the compounds, compositions comprising the compounds, and methods of repelling pests using the compounds and/or compositions.

The present invention relates to a method for the metal-free preparation of a biaryl compound by a photosplicing reaction and its use in the preparation of chemical compounds, preferably of active ingredients e.g. in the fields of pharmaceuticals and agrochemicals. In particular, it refers to a method for the regiocontrolled preparation of a biaryl compound of formula (I): Ar—Ar′ by photochemically reacting a precursor compound of formula (II): Ar—L—Ar′ to form a biaryl compound of general formula: Ar—L—Ar′(II).fwdarw.Ar—Ar′ (I) wherein Ar and Ar′, independently of each other, represent an unsubstituted or substituted C6-C20 aryl group or a heteroaryl group with 5-20 ring atoms selected from carbon, nitrogen, oxygen and sulfur, and L represents a group —X—Y—Z— as defined herein. The biaryl compounds are generally suitable as intermediates or key building blocks in a very broad spectrum of organic chemical syntheses and their respective utilities. Their use within the field of synthesis of active ingredients is an aspect of the invention, and their use in the preparation of pharmaceutically active ingredients is particularly preferred.