11 results about "Cinchona Alkaloids" patented technology

The invention relates to the technical field of scalp care, and discloses a scalp itching relieving composition and application thereof.The scalp itching relieving composition is mainly composed of forsythin, isatis tinctoria extract, cinchona alkaloid, a pH regulator and a solvent and can be used for shampoo, hair conditioners, scalp essence, scalp spray and hair masks. The fructus forsythiae phenol, the isatis tinctoria extract and the cinchona alkaloid in the scalp itching-relieving composition have a remarkable synergistic effect, and the scalp itching-relieving composition is efficient in itching-relieving effect, long-acting, mild, safe, low in irritation and suitable for various scalp types.

Certain embodiments of the present disclosure provide liquid pharmaceutical formulations, suitable for oral administration, that contain from 10 mg / ml to 100 mg / ml of a cinchona alkaloid, a solvent that is at least one of a glycerin, a propylene glycol (PG), and a polyethylene glycol (PEG); and a carbonate. In such formulations, the solvent and the carbonate are present in amounts sufficient to promote resistance to hydrogen peroxide mediated degradation of the cinchona alkaloid.

The invention discloses a method for stereodivergently synthesizing tetra-substituted axially chiral quinolinone. According to the method, MBH carbonate and quinolin-2 (1H)-ketone are used as raw materials, cinchona alkaloid is used as a catalyst, DME is used as a solvent, a quinolinone central chiral compound is synthesized, DBU or sodium methoxide is used as alkali, toluene is used as a solvent, and enantiomer-enriched E-or Z-tetra-substituted axially chiral quinolinone is obtained. The method has the advantages of mild reaction conditions, easily available raw materials, high product enantioselectivity and excellent yield, and provides four stereoisomers (S, E), (R, E), (S, Z) and (R, Z) under specific conditions.

The invention discloses a method for synthesizing a camptothecin chiral precursor with high enantioselectivity, and belongs to the field of organic synthesis. In the invention, the preparation of a chiral precursor amide compound of camptothecin comprises the following steps: synthesizing corresponding aryl (E)-2-ethylbutyl-2-olefine acid ester, mixing the aryl (E)-2-ethylbutyl-2-olefine acid ester with a phase transfer catalyst derived from cinchona alkaloid in an organic solvent, sequentially adding acid, potassium permanganate and a small amount of potassium fluoride solution for reaction, and after the reaction is finished, performing suction filtration to obtain the chiral precursor amide compound of camptothecin. Carrying out amine ester exchange with diethylamine; and evaporating the solvent, and quickly purifying by using a silica gel column to obtain the camptothecin precursor chiral amide compound with high enantioselectivity. The invention aims at providing a new thought and a new method for total synthesis of camptothecin based on a camptothecin chiral precursor reported in literatures, and broadens a synthesis route for synthesizing camptothecin.

This invention discloses an adamantylphosphine ligand with a cinchona alkaloid skeleton, a silver catalyst containing such ligand, and its applications. The ligand has a structure as shown in formula (I) or its tautomers, enantiomers, and diastereomers: In formula (I), R 1 is ethyl or vinyl; the substituent R 2 The novel catalyst, composed of a cinchona alkaloid skeleton adamantylphosphine ligand and a silver salt, can efficiently catalyze the asymmetric [3+2] cycloaddition reaction of aromatic aldehydes and isocyanatoacetic acid esters, obtaining the corresponding chiral oxazoline intermediates with high stereoselectivity and high yield. This technology can be applied to the asymmetric synthesis of florfenicol intermediates and chloramphenicol intermediates, and has the advantages of a short synthetic route, high yield, and good stereoselectivity, thus providing good economic and social benefits.

The invention discloses a method for catalyzing enantioselective ring-opening polymerization of oxygen ring anhydride by using a cinchona alkali derivative, and belongs to the technical field of enantioselective polymerization. The invention solves the problem that the existing catalytic system cannot realize chiral recognition and enantioselective polymerization of the OCA monomer. In a certain solvent and at a certain temperature, a chiral cinchona base catalyst is utilized to catalyze ring-opening polymerization of a chiral substituted OCA monomer to obtain a polyester material with a specific structure. According to the invention, the recognition and enantioselective ring opening polymerization of the chiral OCA by the chiral catalyst are realized for the first time. Different from the traditional OCA stereoselective polymerization which is based on a chain end recognition mechanism, the method disclosed by the invention realizes the process of catalyzing the asymmetric resolution polymerization of the OCA based on enantiomer position point control for the first time. In addition, the catalyst used in the invention has the advantages of commercially available, low price, green and environmental protection.

The invention relates to preparation of a cinchona alkali-metal complex and application of the cinchona alkali-metal complex in an asymmetric cyanidation reaction. The invention belongs to the technical field of fine chemical synthesis. The method comprises the following steps: modifying quinine, quinidine, cinchonine and cinchonidine to introduce an amino group capable of being additionally coordinated to a C9 site, introducing a hydroxyl group capable of being additionally coordinated to a C6 site, reacting the amino group introduced to the C9 site with sulfonyl chloride to introduce more coordination groups, and then coordinating with a cheap alkaline metal reagent to obtain the cinchona alkali-metal complex. The cinchona alkaloid-metal complex catalyst disclosed by the invention can catalyze an asymmetric cyanidation addition reaction of an alpha, beta-unsaturated carbonyl compound to obtain a cyanidation addition product with high enantioselectivity, and is expected to be used as a chiral ligand to realize more asymmetric catalytic reactions; the preparation method disclosed by the invention has the advantages of high yield, low raw material cost, short reaction route, mild reaction conditions and the like, and has a wide application prospect.

The invention relates to a method for catalyzing asymmetric synthesis of a chiral herbicide tetrazolomide, and relates to a herbicide and a synthesis method. The specific method comprises the following steps: catalyzing an asymmetric Michael addition reaction of dithiomalonate and nitroolefin by using a chiral squaramide catalyst based on cinchona alkaloid to obtain a key intermediate, and then carrying out nitro reduction, lactamization, hydrolysis, methylation, amidation and other steps to obtain the dithiomalonate. The chiral tetrazolomide is synthesized with a good total yield and excellent enantioselectivity. The method has the main advantages that the use amount of the chiral catalyst is low, the environmental pollution is reduced by taking water as a solvent, the reaction yield is high, the stereoselectivity is good, the reaction condition is mild, and the post-treatment is simple. The reaction conditions of the method are also suitable for large-scale preparation and industrial production, so that the method has higher application value and social and economic benefits.

The invention discloses a double-bond isomerization catalyst, a preparation method thereof and a double-bond isomerization method, and belongs to the technical field of organic chemical engineering, cinchona alkaloid in the catalyst can promote allylic deprotonation of coordinated olefin so as to accelerate the reaction process, and also can be used as a ligand to be coordinated with a metal atom vanadium to form a complex to act on a substrate, so that the reaction efficiency is improved. The catalyst has double functions of base catalysis and metal catalysis, so that the catalyst has the characteristic of high activity; the magnetic Fe3O4 nanoparticles are adopted as the carrier, so that more active sites can be dispersed on the surface of the catalyst; the cinchona alkaloid is loaded, so that the usage amount is reduced, and recycling of the cinchona alkaloid and separation and purification of a product are facilitated; the double-bond isomerization catalyst is used in double-bond isomerization synthesis, and has the advantages of high reaction catalysis efficiency, short reaction time, high catalytic activity, good selectivity and high yield; the reaction system is a solvent-free system, the post-treatment is simple, and the solvent recovery cost is reduced.

The present application discloses a double-bond isomerization catalyst, a preparation method thereof, and a double-bond isomerization method, which belong to the technical field of organic chemical industry. The cinchona alkaloid in the catalyst can promote the allylic deprotonation of coordinated olefins, thereby accelerating the reaction process. It can also act as a ligand to coordinate with metal atom vanadium to form a complex and act on the substrate, having both base-catalysis and metal-catalysis dual functions, making the catalyst exhibit high activity characteristics. Using magnetic Fe3O4 nanoparticles as the carrier is conducive to the dispersion of more active sites on the surface of the catalyst. Loading the cinchona alkaloid not only reduces the usage amount but also facilitates its recycling and the separation and purification of products. When the double-bond isomerization catalyst is used in the synthesis of double-bond isomerization, the reaction has high catalytic efficiency, short reaction time, high catalytic activity, good selectivity, and high yield. The reaction system is a solvent-free system, with simple post-treatment and reduced solvent recovery cost.

The present application belongs to the technical field of fine chemical synthesis. The purpose of the present application is to solve the technical problems of low yield, long reaction time, harsh reaction conditions and unsuitable for industrial production of the existing asymmetric conjugate cyanation addition reaction method for preparing optically pure beta-cyanoketone. The method of the present application: taking alpha, beta-unsaturated carbonyl compound as the substrate, taking acetone cyanohydrin as the cyan source, under the action of cinchona alkaloid derivatives, alkali and additives, without complicated operation, optically pure beta-cyanoketone is prepared in one step under the heating of nitrogen atmosphere. By screening the cinchona alkaloid derivatives, alkali, additives, reaction temperature and reaction solvent, and coordinating the optimal proportion of each substance, the side reaction is maximally inhibited, and beta-cyanoketone is obtained with high stereoselectivity and yield. The method of the present application has mild conditions, simple operation process and short reaction time, and has wide application prospect.