30results about How to "Conducive to green industrial production" patented technology

The invention provides a preparation method of duloxetine. The method uses 1-naphthol and 3-(2-thienyl)-2-acrolein as starting materials, and obtains (S) through an addition reaction under the action of a catalyst. )-3-(1-naphthyloxy)-3-(2-thienyl) propionaldehyde, then carry out imidization reaction with methylamine, and obtain duloxetine through reduction reaction. The raw materials of the invention are cheap and easy to obtain, do not need expensive 1-fluoronaphthalene, sodium hydride and a cumbersome splitting process, the cost is low, the technological process is safe and easy to operate, the amount of three wastes produced is small, and it is green and environmentally friendly, and the reaction atom economy is high. , the reaction selectivity of each step is high, the side reactions are few, and the optical purity and yield of the target product are high, which is beneficial to the green industrial production.

The invention discloses a simple preparation method of Relebactam intermediate, namely (2S,5R)-N-(1-protective group) piperidine-4-yl-6-benzyloxy-7-oxo-1,6-diazabicyclo[3.2.1]octane - 2- formamide, (2S,5R)-6-benzyloxy-7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carbonyl chloride is prepared from (2S, 5R) -5- benzyloxaminopiperidine -2- formic acid and phosgene, solid phosgene or diphosgene in a solventin the presence of an alkali and a catalyst by epoxidation and acylating chlorination reaction by a one-pot method, and the (2S,5R)-6-benzyloxy-7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carbonyl chlorideis not separated and is directly subjected to amidation reaction with (1-protective group)-4-amino piperidine to obtain the (2S,5R)-N-(1-protective group) piperidine-4-yl-6-benzyloxy-7-oxo-1,6-diazabicyclo[3.2.1]octane - 2- formamide. The method disclosed by the invention is simple in steps, cheap and easily available in raw materials, green and environment-friendly in process, low in cost, high in reaction atom economy, high in purity, yield and selectivity of the obtained intermediate, and beneficial to industrial production.

The invention provides a vitamin A acetate intermediate C15 and a preparation method of vitamin A acetate. The method uses 1-halo-2-methyl-4-acetoxy-2-butene as raw material, and triphenylphosphine or phosphite triester to prepare the corresponding Wittig reagent through substitution reaction, and then react with β-cyclic lemon The aldehyde undergoes Wittig reaction, hydrolyzes the ester group under alkaline conditions, and acidifies to obtain the corresponding halogenated product, and then reacts with triphenylphosphine or phosphite triester again to prepare C15. Vitamin A acetate can be prepared by using the obtained C15 under alkaline conditions and 2-methyl-4-acetoxy-2-butenal through Wittig reaction. The method of the invention has single reaction types, easy operation and realization of reaction conditions, safe and environment-friendly operation, simple post-treatment, and low cost; strong reactivity, high reaction selectivity, high atom economy, and high yield and purity of target products.

The invention relates to an Alectinib intermediate and a preparation method of Alectinib. The method comprises the following steps of: carrying out condensation on 2-nitro-4-cyanophenyl acetate with 2-methyl-2-(4-ethyl-3-substituted)phenyl propionate / propionyl chloride, hydrolyzing ester groups, carrying out amination by dimethylamine hydrochloride, then carrying out a reduction-cyclization reaction to obtain an intermediate 2,3,6-trisubstituted indole derivative, and carrying out a cyclization reaction with a cyclization reagent to prepare Alectinib. The method has the advantages of cheap andeasily-obtained raw materials, short process flow and safe and simple operation; the related unit reactions have high unit reaction selectivity and small waste water amount; and green and simple production of the Alectinib is facilitated.

The invention provides a preparation method of halofantrolene hydrochloride. The method utilizes 4‑trifluoromethyl‑2‑(3,5‑dichlorophenyl) phenylacetic acid to generate corresponding acid chlorides with acyl chloride reagents, and then carry out Friedel-Crafts cyclization, followed by N,N-di-n-butyl Base-β-aminopropionate condensation, and finally through reduction, aromatization, and salt formation to obtain halofantrine hydrochloride. The method of the invention has cheap and easy-to-obtain raw materials and low cost; the reaction conditions are easy to realize, the technological process and operation are safe and convenient, the amount of waste water is generated less, and the method is environmentally friendly; the intermediate has good stability, high reactivity and selectivity, and few side reactions. The preparation of halofantrolene hydrochloride has less impurity, high purity and high yield.

The invention relates to a preparation method of pyridine derivatives. The method uses piperidine-4-one hydrochloride as a raw material to obtain a series of pyridine derivatives through halogenation reaction and elimination reaction. Preparation of 3,5-dihalopiperidin-4-one and 3,3,5-trihalogenated piperidine-4 through halogenation reaction with piperidine-4-one hydrochloride and a specific amount of halogenated reagent -ketone or 3,3,5,5-tetrahalogenated piperidine-4-ketone, and then react with different types of basic reagents to obtain pyridine derivatives whose 4-position is respectively hydroxyl, amino or dimethylamino Elimination reaction. The invention has the advantages of simple and convenient operation, mild conditions, short process flow, low waste water volume, environmental protection and low cost, and is beneficial to the green industrialized production of the pyridine derivatives.