专利号:EP-0542969-B1 优先权日:1991-06-04 标 题:Biodegradable particulate vector and method of synthesis 发明人:SAMAIN DANIEL; DE MIGUEL IGNACIO; MENIALI JAOUAD; IOUALALEN KARIM; DING LI; CERVILLA MONIQUE; RIEUMAJOU VALERIE; DELRIEU PASCAL; IMBERTIE LAURENT 权利人:BIOVECTOR THERAPEUTICS SA 摘要:A biodegradable particulate vector is disclosed and is characterized in that it comprises: a nucleus consisting of a cross-linked polysaccharide or oligosaccharide matrix to which ionic ligands are attached; a first semi-permeable lipid layer linked to the nucleus by covalent bonds; a second layer of amphiphilic compounds linked to the first lipid layer by hydrophobic interactions. A method for synthesis of said vector is also disclosed.
专利号:US-2008280855-A1 优先权日:2005-06-22 标 题 :Process For the Production of Intermediates For the Preparation of Tricyclic Benzimidazoles 发明人:CHIESA MARIA VITTORIA; PALMER ANDREAS; BUHR WILM; ZIMMERMANN PETER JAN; BREHM CHRISTOF; SIMON WOLFGANG-ALEXANDER; POSTIUS STEFAN; KROMER WOLFGANG; ZANOTTI-GEROSA ANTONIO 权利人:NYCOMED GMBH 摘要:The invention relates to a process for the synthesis of compounds of the formula 1-a and compounds of the formula 1-b. n n n n n n n n n n The compounds of the formula 1-a and the compounds of the formula 1-b, in which the substituents R1, R2, R3, and Ar have the meanings indicated in the description, are valuable intermediates for the preparation of pharmaceutically active compounds.
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-5281725-A 优先权日:1991-10-07 标 题:Derivatives of 2,2-dihalogenobenzo[1,3]dioxoles substituted in the 4-position, processes for their preparation and their use 发明人:ANDRES PETER; MARHOLD ALBRECHT 权利人:BAYER AG 摘要:New 2,2-dihalogeno-benzo[1,3]dioxoles substituted in the 4-position, of the general formula (I) ##STR1## in which R represents fluorine, chlorine, bromine or nitro and n Hal represents chlorine or fluorine, and their use as starting substances for the synthesis of highly active compounds, for example in the field of plant protection and pharmaceuticals. n The compounds of the formula (I) can be prepared by analogous processes, for example by chlorination from corresponding benzo[1,3]dioxoles substituted in the 4-position, and these substances according to the invention can be further reacted with hydrogen fluoride to give substances to which the invention likewise relates.
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:US-9233920-B2 优先权日:2010-06-11 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:EL QACEMI MYRIEM; SMITS HELMARS; CASSAYRE JEROME YVES; MULHOLLAND NICHOLAS PHILLIP; RENOLD PETER; GODINEAU EDOUARD; PITTERNA THOMAS; SYNGENTA PARTICIPATIONS AG; SYNGENTA LTD 摘要:The present invention provides stereoselective processes for the preparation of compounds of formula (I) wherein 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; R 1 is chlorodifluoromethyl or trifluoromethyl; R 2 is optionally substituted aryl or optionally substituted heteroaryl; n is 0 or 1; including the process comprising (a-i) reacting a compound of formula II wherein P, R 1 and R 2 are as defined for the compound of formula I; with nitromethane in the presence a chiral catalyst to give a compound of formula III Wherein P, R 1 and R 2 are as defined for the compound of formula I; and (a-ii) reductively cyclizing the compound of formula III to give the compound of formula I. The invention also provides intermediates useful for processes for the synthesis of compounds of formula (I).
1: Brandhorst TT, Klein BS. Uncertainty surrounding the mechanism and safety of the post-harvest fungicide fludioxonil. Food Chem Toxicol. 2019 Jan;123:561-565. doi: 10.1016/j.fct.2018.11.037. Epub 2018 Nov 17. 2: Schnabel G, Tan Q, Schneider V, Ishii H. Inherent tolerance of Colletotrichum gloeosporioides to fludioxonil. Pestic Biochem Physiol. 2021 Feb;172:104767. doi: 10.1016/j.pestbp.2020.104767. Epub 2020 Dec 29. 8(8):839. doi: 10.3390/jof8080839. 4: Graiet I, Hamdi H, Abid-Essefi S, Eyer J. Fludioxonil, a phenylpyrrol pesticide, induces Cytoskeleton disruption, DNA damage and apoptosis via oxidative stress on rat glioma cells. Food Chem Toxicol. 2022 Dec;170:113464. doi: 10.1016/j.fct.2022.113464. Epub 2022 Oct 11. 9(9):500. doi: 10.3390/biom9090500.
合成参考文献
摘要:Franke C et al; Chemosphere 29: 1501-14 (1994) 摘要:Zhang W et al; Environ Monit Assess 187: 4661 (2015) 摘要:S109 | PARCEDC | List of 7074 potential endocrine disrupting compounds (EDCs) by PARC T4.2 | DOI:10.5281/zenodo.10944198 摘要:S132 | UJIGCAPCICCS | A GC-APCI-IMS-HRMS CCS Library from Izquierdo-Sandoval et al. (2022) | DOI:10.5281/zenodo.15831151 参考文献:10.1007/s00438-002-0649-6 摘要:Nakaune R, Hamamoto H, Imada J, Akutsu K, Hibi T. A novel ABC transporter gene, PMR5, is involved in multidrug resistance in the phytopathogenic fungus Penicillium digitatum. Molecular Genetics and Genomics. 2002 Feb 22;267(2):179–85. doi: 10.1007/s00438-002-0649-6.