CAS: 907204-31-3; Fluxapyroxad

硝基氯苯置于10% Pt/activated Carbon,叔丁基二环己基膦,氢气,Palladium Diacetate,Sodium Carbonate,三乙胺体系中,用 环己烷,水,乙酸乙酯 作为反应溶剂,20.0~100.0 °C,1.0 Mpa 条件下,反应 21.67H,反应生成 氟苯吡菌胺
参考文献:Pd催化的suzuki-Miyaura交叉偶联芳基氯在水中低催化剂负载量,用于合成工业上重要的杀菌剂
标题:Pd催化的suzuki-Miyaura交叉偶联芳基氯在水中低催化剂负载量,用于合成工业上重要的杀菌剂
摘要:公开了缺电子芳基氯化物在水中合成作物保护相关活性成分中的 Suzuki-Miyaura 偶联反应.反应条件的优化允许在较短的反应时间内在交叉偶联反应步骤中以 50 Ppm 的 Pd 催化剂负载量进行反应,而无需额外的有机溶剂.该系统针对大规模生产的杀菌剂啶酰菌胺,氟吡菌胺和联苯吡菌胺的初始交叉偶联步骤进行了优化,产率高达 97%.还表明,在后处理中使用对环境无害的溶剂进行简单的产物分离和纯化,可以轻松地将 Suzuki-Miyaura 反应放大到 50 G.为了展示这种方法的可用性,它被额外应用于所需活性成分的三步合成.
DOI:10.1039/d1Gc02602J

专利信息

专利号:US-2022372000-A1
优先权日:2021-05-05
标 题:New Process for the Synthesis of 5-Fluoro-3-(Difuoromethyl)-5-Fluoro-1-Methyl-1H-Pyrazole-4-Carboxylic Acid Derivatives and the Free Acid Thereof
发明人：LUO WEIFEN; WU WENTING
权利人:FUJIAN YONGJING TECH CO LTD
摘要:The invention provides a new process for the synthesis of 5-fluoro-3-(difluoromethyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxylic acid derivatives and the free acid thereof, involving a direct fluorination reaction with a fluorination gas comprising or consisting of elemental fluorine (F2), in a reactor which is resistant to elemental fluorine (F2) and hydrogen fluoride (HF), and wherein in the process as a starting material a difluoromethyl-pyrazole compound dissolved in an inert solvent is subjected to the direct fluorination reaction. Some particular examples of 5-fluoro-3-(difluoromethyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxylic acid derivatives which can be prepared according to the process of the invention are 3-(difluoromethyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxylic acid fluoride (5F-DFMPAF), also known under the alternative name 3-(difluoromethyl)-5-fluoro-1-methyl-1H-pyrazole-4-carbonyl fluoride; 3-(difluoromethyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxylic acid ethylester (5F-DFMP); and 3-(chlorodifluoromethyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxylic acid ethylester (5F-CDFMP), or the corresponding methyl esters. The 5-fluoro-3-(difluoromethyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxylic acid can be obtained from its carboxylic acid derivatives such as, e.g., mentioned before in that the acid derivative is converted to the corresponding carboxylic acid.

专利号:US-12134603-B2
优先权日:2022-08-24
标 题:Synthesis method for N-methyl-3-substituted methyl-4-pyrazolamide derivative and N-methyl-3-substituted methyl-4-pyrazolic acid
发明人：LIU SHENGXUE; SHI YINTAO; GONG QIANG; Zhong Sufang; ZHANG JIANJIANG; QIAN XIAOYUAN; GUO FANG; CHEN RUJUN; JIAN XIAOYING
权利人:SHAOXING SHANGYU XIN YINBANG BIOCHEMICAL CO LTD
摘要:The present application relates to a synthesis method for N-methyl-3-substituted methyl-4-pyrazolamide derivative and N-methyl-3-substituted methyl-4-pyrazolic acid, including the following steps: step S1: synthesis of intermediate E; step S2: synthesis of intermediate D; step S3: synthesis of intermediate C; step S4: synthesis of N-methyl-3-substituted methyl-4-pyrazolamide derivative; and synthesis of N-methyl-3-substituted methyl-4-pyrazolic acid by decomposition of N-methyl-3-substituted methyl-4-pyrazolamide derivative.

专利号:WO-2025056767-A1
优先权日:2023-09-15
标题 :Process for the preparation of enantiomerically enriched aliphatic amines
发明人：BOU HAMDAN FARHAN; GODINEAU EDOUARD; SMEJKAL TOMAS; DUMEUNIER RAPHAEL; BOUSSEMGHOUNE MOHAMED ABDELOUAHAB; BLUM MATHIAS
权利人:SYNGENTA CROP PROTECTION AG
摘要:The present invention relates to a process for the preparation of enantiomerically enriched cyclobutylamines of formula (I) from α-tertiary cyclobutanones and reacting said enantiomerically enriched cyclobutylamines to enantiomerically enriched cyclobutylamides. Such compounds are useful intermediates in the synthesis of microbiocidal thiazole compounds.

专利号:US-2016073631-A1
优先权日:2013-03-04
标 题 :Process for the preparation of dihydropyrrole derivatives
发明人：EL QACEMI MYRIEM; SMITS HELMARS; CASSAYRE JEROME YVES; MULHOLLAND NICHOLAS PHILLIP; RENOLD PETER; GODINEAU EDOUARD; PITTERNA THOMAS
权利人:SYNGENTA PARTICIPATIONS AG; SYNGENTA LTD
摘要:The present invention provides stereoselective processes for the preparation of compounds of formula (I) n n n n n n n n n n n n wherein n P is phenyl, naphthyl, a 6-membered heteroaryl group containing one or two nitrogen atoms as ring members, or a 10-membered bicyclic heteroaryl group containing one or two nitrogen atoms as ring members, and wherein the phenyl, naphthyl and heteroaryl groups are optionally substituted; n R 1 is chlorodifluoromethyl or trifluoromethyl; n R 2 is optionally substituted aryl or optionally substituted heteroaryl; n n is 0 or 1; n including the process comprising n (a-i) reacting a compound of formula II n n n n n n n n n n n n n n n n wherein P, R 1 and R 2 are as defined for the compound of formula I; n with nitromethane in the presence a chiral catalyst to give a compound of formula III n n n n n n n n n n n n n n n n wherein P, R 1 and R 2 are as defined for the compound of formula I; and n (a-ii) reductively cyclising the compound of formula III to give the compound of formula I. n n n n n The invention also provides intermediates useful for processes for the synthesis of compounds of formula (I).

专利号:EP-4378929-A1
优先权日:2022-11-29
标题 :Synthesis of aromatic boronic acids
发明人：KISIN-FINFER EINAT; FALLEK REUT
权利人:ADAMA MAKHTESHIM LTD
摘要:The invention relates to a method for the preparation of phenylboronic acids of formula (I), or combinations thereof, key intermediates in the preparation of compounds of interest in the agrochemical industry. The process comprises adding a borate over a Grignard reagent.

专利号:WO-2024159724-A1
优先权日:2023-02-03
标 题:O-biphenyl oxazoline compound and synthesis method therefor
发明人：ZHU JIANSHE; WANG MINGCHUN; LI QINGYI
权利人:KEYLAB JIANGSU TECH CO LTD
摘要:A synthesis method for an o-biphenyl oxazoline compound. An aryl metal compound as represent by formula II reacts with aryl oxazoline as represented by formula III to generate the o-biphenyl oxazoline compound as represented by formula I. The o-biphenyl oxazoline compound can be used for industrial preparation of o-aminobiphenyl compounds, and used for synthesizing succinate dehydrogenase inhibitor fungicides (IV) such as fluxapyroxad, bixafen, boscalid, and pyraziflumid.