56results about How to "New route" patented technology

The invention provides a new strain-Rhodococcus sp. ZJPH1003 and an application thereof in preparing S-(+)-2,2-dimethylcyclopropane carboxylic acid through microbial catalytic asymmetric hydrolysis of 2,2-dimethylcyclopropane ethyl formate. The strain is conserved at China Center for Type Culture Collection, the conservation address is Wuhan University, Wuhan, China, postcode 430072, the conservation number is CCTCC M 2010371, and the conservation date is December 29, 2010. In the invention, the adopted method for preparing the S-(+)-2,2-dimethylcyclopropane carboxylic acid through microbial catalytic asymmetric hydrolysis of the 2,2-dimethylcyclopropane ethyl formate by utilizing the new microbial strain has the advantages of novel route, high yield, environmental friendliness and the like; and by utilizing a chiral biocatalysis method which takes a Rhodococcus ZJPH1003 cell as a catalyst, for the target product-S-(+)-2,2-dimethylcyclopropane carboxylic acid, the e.e can reach 82.5% and the yield can reach 41.3% when the substrate concentration is 30mmol / L.

The invention discloses a new preparation method of a key intermediate, namely 3-amino-2-hydroxyphenylacetone, for preparation of Pranlukast. The new preparation method comprises the following main steps: taking 2-aminophenol-4-sulfonic acid as a starting raw material, and carrying out acylation, Fries rearrangement, hydrolysis and deprotection, so that 3-amino-2-hydroxyphenylacetone is obtained. Compared with the prior art, the new preparation method disclosed by the invention has the advantages that the used raw materials are cheap and easily available, technology can easily realize industrialization, and the obtained final product is high in purity; no danger technology is adopted, and equipment is simple; and route is novel, and synthesis route is short.

The invention discloses a preparation method of rosuvastatin sodium, comprising the following steps: (4R-Cis)-6-hydroxymethyl-2,2-dimethyl-1,3-dioxane-4- The sulfonylation reaction of tert-butyl acetate and p-toluenesulfonyl chloride under the action of a catalyst gives (4R-Cis)-6-p-toluenesulfonyl-2,2-dimethyl-1,3-dioxane-4 ‑tert-butyl acetate; then react with trimercapto-s-triazine under the action of a basic catalyst to obtain substance A; then oxidize with oxidant to obtain substance B; then react with 4‑(4‑fluorophenyl)‑6‑isopropyl ‑2‑[(N‑Methyl‑N‑methylsulfonyl)amino]pyrimidine‑5‑formaldehyde is reacted under the catalysis of sodium hydride to obtain substance C; finally deprotected by hydrochloric acid, and sodium hydroxide is hydrolyzed into a salt to obtain rosuvastatin sodium.

The invention discloses a quinoid chalcone compound with an isopentenyl group at an A ring, and a preparation method and anti-inflammatory activity thereof. The compound has a structure as shown in a general formula (I) which is described in the specification. The preparation method comprises the following steps: (1) synthesizing 3,5-dihydroxy-2-acetyl-6,6-diisopentenylcyclohexyl-2,4-dienone; (2) synthesizing 3-hydroxy-5-methoxy-2-acetyl-6,6-diisopentenylcyclohexyl-2,4-dienone; (3) synthesizing a methoxy group protected quinoid chalcone compound with the isopentenyl group at the A ring; and (4) synthesizing the quinoid chalcone compound with the isopentenyl group at the A ring. The compound is simple to prepare and has obvious anti-inflammatory action.

The invention discloses a preparation method of pitavastatin calcium intermediate, comprising the following steps: (4R-Cis)-6-hydroxymethyl-2,2-dimethyl-1,3-dioxane-4 The sulfonylation reaction of tert-butyl acetate and p-toluenesulfonyl chloride under the action of a catalyst gives (4R-Cis)-6-p-toluenesulfonyl-2,2-dimethyl-1,3-dioxane- 4-tert-butyl acetate; then react with trimercapto-s-triazine under the action of a basic catalyst to obtain substance A; then oxidize to obtain substance B through the action of an oxidizing agent; finally react with 2-cyclopropyl-4-(4-fluorophenyl ) quinoline-3-formaldehyde is reacted under the catalysis of sodium hydride to obtain pitavastatin calcium intermediate. The raw material of the present invention is cheap and easy to obtain, good atom economy, green and environmental protection, mild and controllable reaction conditions, simple operation, simple purification treatment, suitable for industrial production, good stereoselectivity, high yield, and the prepared pitavastatin calcium intermediate Good purity.

The invention discloses a method for synthesizing Roxatidine intermediate 3-(1-piperidinyl methyl) phenol and relates to the technical field of organic synthesis. M-anisyl alcohol which is cheap and easy to obtain is used as a raw material and firstly reacts with sulfinyl chloride to produce m-methoxybenzyl chloride, then the m-methoxybenzyl chloride reacts with piperidine to produce 3-(1-piperidinyl methyl) anisole, and finally demethoxylation is performed in hydrobromic acid to obtain the target product 3-(1-piperidinyl methyl) phenol. The route is clear, the yield is high, the amount of produced waste water, gas and residues is small, the recycling of solvent can be realized, the preparation cost is reduced and the cost is less than half of the cost of the original route.

The invention provides a preparation method for a key intermediate (I) of letrozole. According to the method, 2-(4-cyanophenyl)formylformic acid (II) and 4-halogenated cyanophenyl (III) are used as raw materials and subjected to one-step reaction in the presence of alkali, a solvent and a catalyst so as to generate a target product. The preparation method is novel in route, simple and controllable in operation, high in reaction yield, economical and capable of ensuring that high-purity letrozole is obtained through subsequent preparation, and provides guarantees for industrial large-scale production of high-purity letrozole.