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三氟乙酰氯置于水体系中,化学反应 2.0H,反应生成 三氟乙酸
参考文献:一种三氟乙酸的制备方法
标题:一种三氟乙酸的制备方法
摘要:本发明公开了一种三氟乙酸的制备方法,包括如下步骤:(1)1,1,1‑三氟‑2‑氯乙烷和氯气汽化后进入装有催化剂的固定床反应器,气相氯化反应合成1,1,1‑三氟‑2,2‑二氯乙烷;(2)1,1,1‑三氟‑2,2‑二氯乙烷和氧气汽化后,在光源作用下氧化反应得到三氟乙酰氯,未反应的1,1,1‑三氟‑2,2‑二氯乙烷冷凝后返回到反应器;(3)三氟乙酰氯水解得到三氟乙酸.本发明具有工艺简单,收率高,三废少等优点,而且反应转化率高,选择性高,反应连续生产,安全环保.

专利信息

专利号:WO-2013138200-A1
优先权日:2012-03-13
标 题 :Green chemistry synthesis of the malaria drug amodiaquine and analogs thereof
发明人：FORTUNAK JOSEPH MARIAN; KULKARNI AMOL ANANT; KING CHRISTOPHER
权利人:UNIV HOWARD
摘要:Methods are provided for a green chemistry one-pot synthesis of amodiaquine and amodiaquine analogs. The methods have a lower environmental impact, lower investment cost, reduced amounts of byproducts and impurities, and a shorter synthesis time, compared to current conventional synthesis methods. The methods reduce the total number of steps in the synthesis from four to five down to two, thereby simplifying production; and allow a reduced number of solvents and reagents to be used in production, thereby reducing the waste generated in the synthesis. The methods can reduce the waste to about 3-5 kilograms of waste generated per kilogram of product produced; and surprisingly improve the overall yield from 60-65% to greater than 90% as compared to the current conventional synthesis methods for amodiaquine and its analogs.

专利号:US-2024409495-A1
优先权日:2021-10-20
标 题 :Process for the preparation of 2,7-dihydroxy-9-fluorenone useful for the synthesis of tilorone and its salts
发明人：JAISANKAR PARASURAMAN; DEB INDUBHUSAN; BHATTACHARJEE PINAKI
权利人:COUNCIL SCIENT IND RES
摘要:Methods involving preparation of building blocks of 2,7-dihydroxy-9-fluorenone toward the synthesis of tilorone dihydrochloride salt and other salts (bromide, iodide, fluoride, citrate, oxalate, maleate, phosphate, tartrate, triflate, trifluoroacetate, tetrafluoroborate) of tilorone, and an efficient, safe, cost effective method for the preparation of 2,7-bis-[2-(diethylamino)ethoxy]-fluorenone-9 and its various salts are developed. The methods involve oxygenation of fluorene, nitration of fluorenone, followed by reduction and diazotization toward the formation of 2,7-dihydroxy-9-fluorenone, which is the key intermediate for the formation of 2,7-bis-[2-(diethylamino)ethoxy]-9-fluorenone-dihydrochloride (Tilorone dihydrochloride) and other tilorone salts. The synthesis method has relatively simple operation, mild reaction conditions, high yield, and simple process with yields of 80-97%. Subsequent product purification of this method uses filtration and crystallization methods, avoiding the existing methods of column chromatography. Therefore, the research of its synthetic method being with a wide range of applications from the drug development and material synthesis point of view.

专利号:US-7420052-B2
优先权日:2001-08-24
标 题:Intermediates for synthesis of vinblastine, process for preparation of the intermediates and process for synthesis of vinblastines
发明人：FUKUYAMA TOHRU; TOKUYAMA HIDETOSHI; YOKOSHIMA SATOSHI
权利人:JAPAN SCIENCE & TECH AGENCY
摘要:An intermediate for vinblastine synthesis represented by general formula A. n ngeneral formula A.n n(in the formula, R 1 , R 2 , R 3 and R 4 are the group selected independently from the group consisting of H, lower alkyl group, lower alkoxy group, halogen, lower perfluoroalkyl group, lower alkylthio group, hydroxy group, amino group, mono- or di-alkyl or acylamino group, lower alkyl or arylsulfonyloxy group. R 5 is H, or a lower alkyl group or a substituted or non-substituted aryl group, R 6 is an alkyl group of carbon number 4 or less, R 7 is a substituted or non-substituted aryl group, R 8 is a substituted or non-substituted aryl group or lower alkyl group and R 9 is an acyl group or trialkylsilyl group.) A method for synthesis of the compound of general formula A utilizing radical ring forming reaction of thioanilides and using the compound of general formula B as the starting material, synthesizing thioanilide of general formula C by the reaction with compound 1 and the formation of a 11-membered ring by intramolecular alkylation of 2-nitrobenzenesulfonamide by which the reactions can proceed under mild conditions and high yield can be accomplished.

专利号:WO-2023030277-A1
优先权日:2021-08-30
标 题:Method for fully liquid-phase synthesis of grnh nonapeptide amide analog
发明人：SUN PENGCHENG; PAN JING; WU JUNYONG; TANG YONGBO; Du Yixiong; GUO LIN
权利人:HUNAN MICRO PEPTIDE BIOMEDICAL CO LTD
摘要:Provided is a method for fully liquid-phase synthesis of a GRnH nonapeptide amide analog, which belongs to the technical field of medicine synthesis. The method comprises respectively synthesizing a 'Trp-Ser-Tyr' fragment, an 'R-Leu' fragment, a 'Pyr-His' fragment and 'Arg-Pro-Hunan T', wherein, R = D-Ala (alarelin), D-Leu (leuprorelin), D-Trp (deslorelin) and D-His (histrelin), and obtaining the GRnH nonapeptide amide analog with high yield and high purity by means of a '3 +2 +2 +2' fragment condensation method. The synthesis method is environmentally friendly, mild, and free of any highly toxic and poisonable reagents. The cost is greatly reduced and the synthesis method is very suitable for large-scale production.

专利号:WO-2025053792-A1
优先权日:2023-09-06
标题:Collective synthesis of phantomolin family through total synthesis of the sesquiterpene lactone molephantin
发明人：CHIBA SHUNSUKE; PATOURET REMI HENRI LOUIS; LI HOI YEUNG; LAI SOAK KUAN
权利人:UNIV NANYANG TECH
摘要:Disclosed herein are processes to generate an intermediate in the total synthesis of (+)- molephantin or a derivative thereof, and a total synthesis of (+)-molephantin or a derivative thereof. Also disclosed herein are methods of forming a compound of formula XIV and of forming a compound of formula XV, wherein compound of formula XIV and compound of formula XV are as defined in the description.

专利号:WO-9740025-A1
优先权日:1996-04-19
标 题 :Solid phase and combinatorial synthesis of substituted 1,2,3-triazoles and of arrays of substituted 1,2,3-triazoles
发明人：DOERWALD FLORENCIO ZARAGOZA
权利人:NOVO NORDISK AS; DOERWALD FLORENCIO ZARAGOZA
摘要:A solid phase method for the synthesis of a plurality of differently substituted 1,2,3-triazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 1,2,3-triazoles are prepared by acylation of a substrate-bound primary or secondary amine with a 3-oxoalkanoic acid and reaction of the resulting amide with a primary amine under dehydrating conditions to give an enamine. Treatment of this substrate-bound enamine with a sulfonyl azide in the presence of a base gives the corresponding 1,2,3-triazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 1,2,3-triazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse triazole-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.