6results about How to "Short route" patented technology

This invention discloses a chemical-biological fusion method for cholesterol synthesis. Using plant-derived 21-hydroxy-20-methylpregn-4-en-3-one, also known as bis(2-hydroxy-2-yl)-3-one (BA), as a raw material, cholesterol is synthesized through a four-step reaction involving sulfonation, acetylation, enzymatic hydrolysis and reduction, and Grignard coupling. Addressing the drawbacks of traditional animal-derived cholesterol, which carries unpredictable risks of pathogenic bacteria and viruses, this invention uses plant-derived steroidal raw material BA to synthesize cholesterol. This method not only offers high safety, avoiding the risk of pathogenic bacteria and viral infections, but also utilizes the tandem catalysis of esterase and carbonyl reductase during synthesis, along with coenzyme regeneration, to obtain key intermediates with high stereoselectivity and in a safe and clean manner. This significantly shortens the cholesterol synthesis route, increases efficiency, simplifies operation, minimizes solvent recycling losses, reduces waste, and allows for mild reaction conditions. This method is safe, economical, and suitable for industrial production.

An amide-containing aromatic diamine has the following structural formula: where Ar is a group with an aromatic ring structure. The preparation method includes the following steps: (1) mixing and reacting components including aromatic diamine, p-nitrobenzoic acid, alkyl phosphoric anhydride and polar aprotic organic solvent; (2) adding carboxylic acid and halogen-free quaternary ammonium salt to the product obtained in step (1) to obtain a mixed solution, which is placed in the cathode cell of an H-type electrolytic cell; the anode cell and the cathode cell are separated by a Nafion membrane; adding the same polar aprotic organic solvent and halogen-free organic electrolyte as the cathode cell to the anode cell of the H-type electrolytic cell, and adding a metal ion-free reducing agent; and conducting the reaction by electrolysis; (3) purifying the cathode reaction solution obtained in step (2) by post-treatment to obtain the amide-containing aromatic diamine. The yield, purity and whiteness of the amide-containing aromatic diamine are higher.

The application discloses givinostat and a synthesis method thereof, wherein compound 1 is used for synthesizing compound 2 in step 01; compound 3 is used for synthesizing compound 4 in step 02; compound 4 is used for synthesizing compound 5 in step 03; compound 5 is used for synthesizing compound 6 in step 04; and compound 6 and compound 2 are used for synthesizing givinostat in step 05. After optimization, the yield of compound 1 to compound 2 reaches more than 80 %, raw materials and reagents used in the reaction are cheap and easy to obtain, and the preparation cost is very low; only four steps are needed from compound 3 to the target product, the route is short, and the operation is simple; and after optimization, the total yield of compound 3 to the target product reaches more than 40 %, the yield is high, and the preparation cost is significantly reduced.

The present application relates to a kind of devices and refining methods for removing acetal in ethanol, device includes the light tower (2) of removal, acetal removal tower (3) and refining tower (4) connected in sequence by pipeline, the light tower (2) of removal is used to separate out light component in the system to be separated, the acetal removal tower (3) is used to separate out acetal, ethyl ester in the system to be separated, the refining tower (4) is used to separate out ethanol rectification and purify in the system to be separated.Compared with prior art, the present application is developed by special acetal removal tower, acetal is removed by using the method of negative pressure rectification, so that its content is reduced to 150ppm below, meet the quality requirements of high-purity ethanol.

The application belongs to the field of pharmaceutical chemical synthesis, and particularly relates to a preparation method of a varenicline intermediate. The method comprises the following steps: 1) in the presence of an organic solvent A, a compound of formula 4 is used as raw material, ammonium acetate and a reducing agent are added, and a compound of formula 3 or a salt thereof is obtained through reaction; 2) in an organic solvent B, the compound of formula 3 or the salt thereof is reacted with trifluoroacetic anhydride or trifluoroacetic ethyl ester under the action of a base to obtain a compound of formula 2; and 3) in the presence of a solvent C and a catalyst, the compound of formula 2 is subjected to nitration reaction with a nitrating agent to obtain a compound of formula 1. The application solves the problems of the prior art, such as complicated steps, low atom utilization rate, high cost and the like, provides a novel route, directly introduces an amino group, does not need to be deprotected, has good atom economy, has mild reaction conditions, is simple in post-treatment, and is suitable for industrial production.

The invention provides a preparation method of bepedioic acid and an intermediate thereof, the preparation method of the bepedioic acid comprises the following steps: reacting a compound 4 with a compound 5 in the presence of alkali to obtain a compound 6, and hydrolyzing the compound 6 and removing a hydroxyl protecting group to obtain the bepedioic acid, and the reaction formula is shown in the specification. The preparation method of the bepedioic acid is short in route, low in cost, high in yield of each step of reaction, few in by-products and suitable for industrial large-scale production.