- Radiochemical Synthesis and Evaluation of 13N-Labeled 5-Aminolevulinic Acid for PET Imaging of Gliomas
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The endogenous amino acid, 5-aminolevulinic acid (5-ALA), has received significant attention as an imaging agent, including ongoing clinical trials for image-guided tumor resection due to its selective uptake and subsequent accumulation of the fluorescent protoporphyrin IX in tumor cells. Based on the widely reported selectivity of 5-ALA, a new positron emission tomography imaging probe was developed by reacting methyl 5-bromolevulinate with [13N] ammonia. The radiotracer, [13N] 5-ALA, was produced in high radiochemical yield (65%) in 10 min and could be purified using only solid phase cartridges. In vivo testing in rats bearing intracranial 9L glioblastoma showed peak tumor uptake occurred within 10 min of radiotracer administration. Immunohistochemical staining and fluorescent imaging was used to confirm the tumor location and accumulation of the tracer seen from the PET images. The quick synthesis and rapid tumor specific uptake of [13N] 5-ALA makes it a potential novel clinical applicable radiotracer for detecting and monitoring tumors noninvasively.
- Pippin, Adam B.,Voll, Ronald J.,Li, Yuancheng,Wu, Hui,Mao, Hui,Goodman, Mark M.
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Read Online
- Selective bromination of ketones. A convenient synthesis of 5-aminolevulinic acid
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Bromination of unsymmetrical ketones with Br2 in methanol proceeded regioselectively in good yield at the less substituted methyl carbon. The bromination of levulinic acid using this method was followed by azidation and amination to lead to an efficient three-step synthesis of 5-aminolevulinic acid in 36% overall yield.
- Ha,Lee,Ha,Park
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Read Online
- Synthesis and characterization of altaicadispirolactone
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Altaicadispirolactone was synthesized via a simple route. In this route, levulinic acid was used as a starting material, and bromination followed by hydrolysis and BF3·OEt2-catalyzed cyclization were carried out. A single-crystal ORTEP drawing has been created and more detailed crystallographic data of the compound has been obtained from X-ray analysis. Copyright Taylor & Francis, Inc.
- Zhang, Yan,Wu, Linbo,Li, Feng,Li, Bo-Geng
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Read Online
- Preparation method 5 - ALA intermediate 5 - bromoolevulinic acid ester
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The invention relates to a preparation method of 5 - ALA intermediate 5 - bromoacetyl ester, which is characterized by comprising the following steps: (S1) reaction of the urotropine and a bromine source to prepare the urotropine bromine complex. (S2) Lourotropine bromide complex and levulinic acid ester reaction. Gave 5 - bromoolevulinic acid ester. Compared with the prior art, a bromo reagent such as liquid bromine and 5 - is used directly, NBS-site bromination product yield is increased 5 - 10% or more. The defect that 3 -position bromination or multi-site bromination product is large and separation is difficult in the bromination reaction is overcome. The method is cheap and easily available in raw materials, simple and convenient to operate and suitable for large-scale preparation 5 - ALA intermediate 5 - bromolevulinic acid ester .
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Paragraph 0028-0030; 0039-0054
(2021/09/22)
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- N-(1H-IMIDAZOL-2-YL)BENZAMIDE COMPOUND AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME AS ACTIVE INGREDIENT
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N-(1H-imidazol-2-yl)benzamide compound of formula (I), or a pharmaceutically acceptable salt, a prodrug, a solvate, or a stereoisomer thereof which is a novel compound exhibiting excellent inhibitory activity against IRAK-4, can be used without side effects for efficient prevention and treatment of diseases mediated by IRAK-4 receptors, particularly autoimmune diseases or lymphomas.
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Page/Page column 43; 45; 152; 159
(2021/04/10)
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- DIHYDROPYRIMIDINE DERIVATIVES AND USES THEREOF IN THE TREATMENT OF HBV INFECTION OR OF HBV-INDUCED DISEASES
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The application describes dihydropyrimidine derivatives which are useful in the treatment or prevention of HBV infection or of HBV-induced diseases, more particularly of HBV chronic infection or of diseases induced by HBV chronic infection, as well as pharmaceutical or medical applications thereof.
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Page/Page column 61-62
(2020/01/24)
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- Synthesis of 5-aminolevulinic acid with nontoxic regents and renewable methyl levulinate
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Synthesis of 5-aminolevulinic acid (5-ALA) was presented with novel bromination of biobased methyl levulinate (ML), followed by ammoniation and hydrolysis. Copper bromide (CuBr2) was employed as the bromination reagent with higher selectivity and activity instead of the conventional liquid bromine (Br2). 5-ALA was obtained in a high yield (64%) and purity (>95%) by optimum design, which is of great potential in industrialization.
- Zai, Yuxia,Feng, Yunchao,Zeng, Xianhai,Tang, Xing,Sun, Yong,Lin, Lu
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p. 10091 - 10093
(2019/04/10)
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- Structure-activity relationship study of thiazolyl-hydroxamate derivatives as selective histone deacetylase 6 inhibitors
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Several human diseases are associated with aberrant epigenetic pathways mediated by histone deacetylases (HDACs), especially HDAC6, a class IIb HDACs, which has emerged as an attractive target for neurodegenerative and autoimmune disease therapeutics. In a previous study, we developed the novel HDAC6-selective inhibitor 9a ((E)-N-hydroxy-4-(2-styrylthiazol-4-yl)butanamide) and showed that it has anti-sepsis activity in vivo. In this study, we conducted structure-activity relationship (SAR) studies to optimize the activity and selectivity of HDAC6, synthesizing its derivatives with various aliphatic linker sizes and cap structures. We identified 6u ((E)-N-hydroxy-3-(2-(4-fluorostyryl)thiazol-4-yl)propanamide), which has nanomolar inhibition activity and a 126-fold selectivity for HDAC6 over HDAC1. Through the docking analyses of 6u against HDAC subtypes, we revealed the importance of the optimal aliphatic linker size, as well as the electronic substituent effect and rigidity of the aryl cap group. Thus, we suggest a new rationale for the design of HDAC6-selective inhibitors.
- Nam, Gibeom,Jung, Jun Min,Park, Hyun-Ju,Baek, Seung Yeop,Baek, Ki Seon,Mok, Hui yeon,Kim, Da Eun,Jung, Young Hoon
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p. 3408 - 3420
(2019/06/25)
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- Method for manufacturing methyl 5-bromolevulinate and manufacturing method 5-aminolevulinic acid heyl ester hydrochloride using the same
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The present invention relates to a method of preparing methyl 5-bromolevulinate, capable of improving the yield of a final product while having stability of a product, and a method of preparing 5-aminoalkylenic acid hexyl ester hydrochloride using the same. To this end, the method of preparing methyl 5-bromolevulinate comprises: a first reaction step of mixing levulinic acid, methanol and bromine in a container and making the mixture react; a second reaction step of mixing a first product of the first reaction step, a first reactant not reacting in the first reaction step, ultrapure water and chloroform solution, and making the mixture react; an extraction step of extracting a chloroform solution layer from a first mixture formed after the second reaction step; a third reaction step of mixing the chloroform solution layer extracted in the extraction step, ethyl ether, and sodium bicarbonate saturated aqueous solution and stirring the mixture; a purification step of separating an aqueous solution layer from a second mixture formed after the third reaction step; a fourth reaction step of mixing a remaining mixture after the aqueous solution layer is separated from the second mixture with N-Hexane, and making the mixture react; a precipitation step of precipitating methyl 5-bromolevulinate in a solid state from a third mixture while quenching the third mixture formed after the fourth reaction step; and a filtering step of filtering the methyl 5-bromolevulinate in the solid state from a fourth mixture formed after the precipitation step by using a filtration device.COPYRIGHT KIPO 2019
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Paragraph 0019-0021
(2019/02/28)
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- Preparation method of 5-haloacetyl propionate
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The invention discloses a preparation method of 5-haloacetyl propionate. Acetylpropionic acid or acetyl propionate and a halogenating agent are taken as raw materials, and the halogenating agent includes NBS (N-Bromosuccinimide), NCS (N-Chlorosuccinimide), ferrous bromide, iron bromide, aluminum bromide, phosphorus tribromide, copper bromide and copper chloride. The acetylpropionic acid or acetylpropionate obtained by hydrolysis of biomass is taken as a raw material, and undergoes a halogenation reaction in the presence of a halogenating agent to synthesize the 5-haloacetyl propionate. The selected raw materials are wide in sources, cheap and readily available; the reaction conditions are mild, and the reaction yield and selectivity are high; moreover, the selected halogenating agent serving as a raw material is less toxic and more environmentally friendly than liquid bromine used in the traditional mercury process, and has a good industrial application prospect.
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Paragraph 0024-0041; 0051-0058
(2018/10/19)
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- Multifunctional Cyclopentadienes as a Scaffold for Combinatorial Bioorganometallics in [(η5-C5H2R1R2R3)M(CO)3] (M=Re, 99mTc) Piano-Stool Complexes
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Multifunctional cyclopentadiene (Cp) ligands and their rhenium and 99mTc complexes were prepared by a versatile synthetic route. The properties of these Cp ligands can be tuned on demand, either during their synthesis (variation of R1) or through post-synthetic functionalization with two equal or different vectors (V1 and V2). Variation of these groups enables a combinatorial approach in the synthesis of bioorganometallic complexes. This is demonstrated by the preparation of Cp ligands containing both electron-donating and electron-withdrawing groups at the R1 position and their subsequent homo- or heterofunctionalization with biovector models (benzylamine and phenylalanine) under standard amide bond-formation conditions. All ligands can be coordinated to the fac-[Re(CO)3]+ and fac-[99mTc(CO)3]+ cores to give tetrafunctional complexes in straightforward and functional-group-tolerant procedures. The 99mTc complexes were prepared in one step, in 30 min, and under aqueous conditions from generator-eluted [99mTcO4]?.
- Frei, Angelo,Spingler, Bernhard,Alberto, Roger
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supporting information
p. 10156 - 10164
(2018/07/29)
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- Carbon nanosphere supported Ru catalyst for the synthesis of renewable herbicide and chemicals
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A carbon nanosphere supported Ru (Ru-CNS) effectively catalyzed the conversion of biorenewable platform chemicals to 5-aminoleulininc acid (ALA), furan alcohols and γ-valerolactone (GVL). The catalyst exhibits high activity for the investigated processes, enabling 76% ALA and > 90% furan alcohols and GVL from their precursors. The effect of solvent polarity on the yield and selectivity of GVL and its ring-opening product has been studied with detailed characterization of the catalyst.
- Gupta, Dinesh,Saha, Basudeb
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p. 206 - 209
(2017/07/18)
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- (HMe 2 SiCH 2) 2: A Useful Reagent for B(C 6 F 5) 3 -Catalyzed Reduction-Lactonization of Keto Acids: Concise Syntheses of (-)- cis -Whisky and (-)- cis -Cognac Lactones
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(HMe 2 SiCH 2) 2 has been utilized as a useful reagent for B(C 6 F 5) 3 -catalyzed reduction-lactonization of keto acids to synthesize γ- and δ-lactones. The process led concisely to (-)- cis -whisky and (-)- cis -cognac lactones in respective overall yields of 32% and 36%.
- Xie, Hengmu,Lu, Ji,Gui, Yingying,Gao, Lu,Song, Zhenlei
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supporting information
p. 2453 - 2459
(2017/10/06)
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- 5-[(PIPERAZIN-1-YL)-3-OXO-PROPYL]-IMIDAZOLIDINE-2,4-DIONE DERIVATIVES AS ADAMTS INHIBITORS FOR THE TREATMENT OF OSTEOARTHRITIS
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The present invention discloses compounds according to Formula (I), wherein R, R2, R3a, R3b, and Cy are as defined herein. The present invention discloses compounds inhibiting ADAMTS, methods for their production, pharmaceutical compositions comprising the same and methods for the prophylaxis and/or treatment of inflammatory conditions and/or diseases involving degradation of cartilage and/or disruption of cartilage homeostasis.
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Paragraph 0271
(2016/07/27)
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- Synthesis of diverse acyclic precursors to pyrroles for studies of prebiotic routes to tetrapyrrole macrocycles
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A chemical model for the origin of tetrapyrrole macrocycles under prebiotic conditions entails the condensation of acyclic dicarbonyl compounds and α-aminoketones to form pyrroles that are equipped for subsequent self-condensation. Development and exploration of the scope of the chemical model (including combinatorial reactions, studies of the effects of structurally defective substrates, and reactions in aqueous or organic media) have relied on the availability of diverse starting materials prepared by traditional chemical synthesis methods. Here the synthesis of all acyclic dicarbonyl compounds and α-aminoketones used in the prior prebiotic model studies is described. There are five sets of acyclic dicarbonyl compounds including (i) β-ketoesters bearing diverse 4-substituents, (ii) levulinic acid derivatives bearing selected 5-substituents (i.e., analogues of δ-aminolevulinic acid, ALA), (iii) meso-substituted β-ketoesters, (iv) meso-substituted β-diketones that contain one 4-substituent, and (v) hybrid molecules that contain both the β-ketoacyl unit and the levulinic acid skeleton (or homologue thereof). A variety of α-aminoketones (homologues of ALA) also have been prepared. Altogether, the synthesis of 53 compounds is described, encompassing 28 new compounds as well as 25 known compounds that have been more fully characterized or prepared via alternative routes. The ability to convert selected acyclic compounds directly via pyrroles to porphyrinogens in a single-flask process may also prove useful in mainstream syntheses of diverse tetrapyrroles regardless of possible prebiotic relevance.
- Chandrashaker, Vanampally,Ptaszek, Marcin,Taniguchi, Masahiko,Lindsey, Jonathan S.
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p. 8786 - 8808
(2016/10/13)
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- A versatile δ -aminolevulinic acid (ALA)-cyclodextrin bimodal conjugate-prodrug for PDT applications with the help of intracellular chemistry
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Grafting of aδ-aminolevulinic acid (1) moieties on the narrow periphery of a β-cyclodextrin (β-CD) derivative through hydrolysable bonds was implemented, in order to generate a water-soluble, molecular/drug carrier with the capacity to undergo intracellular transformation into protoporphyrin IX (PpIX), an endogenous powerful photosensitizer for photodynamic therapy (PDT). The water-soluble derivative 2 was prepared by esterifying aδ-azidolevulinic acid with heptakis(6-hydroxyethylamino-6-deoxy)-β- cyclodextrin, with an average degree of substitution, DS = 3. Delivery of water-soluble, colorless 2 to cells resulted in intense red fluorescence registered by confocal microscopy, evidently due to the engagement of the intracellular machinery towards formation of PpIX. Conjugate 2 was further complexed with a fluorescein-labeled model guest molecule which was successfully transported into the cells, thereby demonstrating the bimodal action of the derivative. The present work shows the versatility of CDs in smart applications and constitutes advancement to our previously shown PpIX-β-CD conjugation both in terms of water solubility and lack of aggregation. lack of aggregation.
- Aggelidou, Chrysie,Theodossiou, Theodossis A.,Gonalves, Antonio Ricardo,Lampropoulou, Mariza,Yannakopoulou, Konstantina
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p. 2414 - 2420
(2015/02/05)
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- Ionic liquids - Advanced reaction media for organic synthesis
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The advantages in the application of ionic liquids as reaction media in organic synthesis, i.e., in the preparation of chromane derivatives, substituted pyrazines, 4-aminofuran-2(5H)-ones, or in bromination of Levulinic acid or dehydration of alcohols, saccharides, and polysaccharides, have been demonstrated on several examples. Ionic liquids with Bronsted acidity have been shown to possess catalytic activity and provide access to convenient technologies for the preparation of various useful compounds. Copyright Merck KGaA.
- Ignat'ev, Nikolai V.,Schulte, Michael,Koppe, Karsten,Barthen, Peter,Zlotin, Sergei G.,Makhova, Nina N.,Sheremetev, Aleksei B.,Valente, Anabela A.
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scheme or table
p. 1205 - 1216
(2011/09/16)
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- HERBICIDALLY ACTIVE HETEROARYL-SΥBSTITΥTED CYCLIC DIONES OR DERIVATIVES THEREOF
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The invention relates to a compound of formula (I), which is suitable for use as a herbicide wherein G is hydrogen or an agriculturally acceptable metal, sulfonium, ammonium or latentiating group; Q is a unsubstituted or substituted C3-C8 saturated or mono-unsaturated heterocyclyl containing at least one heteroatom selected from O, N and S, or Q is heteroaryl or substituted heteroaryl; m is 1, 2 or 3; and Het is an optionally substituted monocyclic or bicyclic heteroaromatic ring; and wherein the compound is optionally an agronomically acceptable salt thereof.
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Page/Page column 89
(2011/02/24)
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- Exploration of novel 2-alkylimino-1,3-thiazolines: T-type calcium channel inhibitory activity
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We have developed combinatorial libraries of new 2-alkylimino-1,3- thiazolines with four diversity points, consisting of more than 500 compounds, in a parallel synthetic fashion. The synthetic strategy was based on the construction of a large library aimed at the discovery of new compounds with T-type calcium channel inhibitory activity through structure modifications of hit compound 2. The syntheses of the compounds of Chemset A with four diversity points were accomplished by the condensation of thioureas 5 with α-haloketones 6{1-66} having two diversity points each. A library of phthalimidyl 1,3-thiazolines 24 was synthesized to provide Chemset B, which allowed the introduction of other diversity points through the nucleophilic character of the amino nitrogen. A sublibrary, Chemset C, was constructed from the libraries of Chemset A and Chemset B by functionalization of the C-4 position of the 1,3-thiazoline ring. The products containing ester or acid groups at the C-4 position of the 1,3-thiazoline ring were used in amide synthesis to give a new sublibrary within Chemset C. Deprotection of the phthalimidyl moiety of 24 followed by the reaction with benzoyl chloride gave the corresponding sublibrary in Chemset C. Another sublibrary which includes secondary amino derivatives was obtained by reduction of the amide moiety or reductive amination of 23 with phenyl aldehyde. The selected compounds from the generated libraries were evaluated with respect to inhibition of T-type calcium channels, where some of them have exhibited promising activity.
- Han, Minsoo,Nam, Kee Dal,Shin, Dongyun,Jeong, Nakcheol,Hahn, Hoh-Gyu
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experimental part
p. 518 - 530
(2010/08/20)
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- Variation in the regioselectivity of levulinic acid bromination in ionic liquids
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The reaction of levulinic acid and its esters with bromine in ionic liquids results in the formation of 3-bromo derivatives as the major products and not the 5-bromo substituted isomers, which are typically formed in organic solvents. The bromination of l
- Zavozin, Alexander G.,Kravchenko, Natalya E.,Ignat'ev, Nikolay V.,Zlotin, Sergei G.
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scheme or table
p. 545 - 547
(2010/10/02)
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- 2-AMINOPYRIDINE ANALOGS AS GLUCOKINASE ACTIVATORS
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Provided are compounds of formula I that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes meilitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.
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(2009/07/03)
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- Synthesis of novel and stable 5-aminolevulinic acid derivatives for the efficient synthesis of 5-aminolevulinic acid based prodrugs
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The efficient synthesis of two stable, easily handled precursors of 5-aminolevulinate is reported. These precursors are stable to the chemical transformation needed for the synthesis of bioconjugates and can be readily deprotected in good yields. Georg Th
- Vallinayagam, Ramakrishnan,Bertschy, Hugo,Berger, Yann,Wenger, Virginie,Neier, Reinhard
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p. 3731 - 3735
(2008/09/19)
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- On the synthesis of cepacin A
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Efforts directed toward a total synthesis of cepacin A is presented in full detail. The C-7, C-8, and C-9 stereogenic centers in the target molecule were derived from d-arabinose. The configuration of the allene axis was controlled at the bromoallenation step by the C-10 configuration of the precursor. An unexpected yet very interesting phenomenon was observed with the bromoallenation, where the α-isomer of the propargylic alcohol 31 was entirely resistant to the conditions that worked so well for its β-counterpart. The problem was eventually solved by careful tuning of the size of the neighboring groups based on the clue obtained from conformational analysis. The diyne moiety was incorporated into the molecular framework through a coupling of the TMS protected diyne with a proper bromoallene under the Sonogashira conditions with EtOAc as the solvent. Use of other solvents at this step led to complete failure.
- Tang, Chao-Jun,Wu, Yikang
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p. 4887 - 4906
(2008/02/01)
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- PROCESS FOR THE PREPARATION OF ALKYL 5- (DICARBOXIMIDO) LEVULINATE AND ALKYL 4-OXO-PENTENOATE
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A method of manufacturing esters of dicarboxyimidolevulinic acid and alkyl trans-4-oxo-2-pentenoate. This method includes two reaction steps, wherein the first step of said two reaction steps is a bromination of alkyl-levulinate, to obtain alkyl-(3 and 5)-bromolevulinate, and the second step of said two reaction steps is a synthesis of esters of dicarboxyimidolevulinic acid and alkyl trans-4-oxo-2-pentenoate, by reacting the alkyl-(3 and 5)-bromolevulinate obtained in said first step with dicarboxyimide anion.
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(2008/06/13)
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- Stereoselective syntheses of dihydroxerulin and xerulinic acid, anti-hypocholesterolemic dyes from the fungus Xerula melanotricha
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The title compounds 2 and 3, which are inhibitors of the biosynthesis of cholesterol, were synthesized in a convergent and perfectly stereoselective manner. In the key step, bromobutenolide 6 (obtained from levulinic acid in two steps) was coupled with either of the novel bis(stannanes) trans,cis, -trans-35 or trans,trans,trans-35 [each accessible from 3-(tributylstannyl)allyl alcohol (17) in four steps], giving γ-alkylidenebutenolide trans,trans,trans-32. This compound was coupled with iododiyne 42 or the bromoenediynoate 44 leading to dihydroxerulin (2) and to the (trimethylsilylethyl)ester 45 of xerulinic acid, respectively. Deprotection of the latter provided totally synthetic xerulinic acid (3) for the first time.
- Sorg, Achim,Siegel, Konrad,Brueckner, Reinhard
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p. 1610 - 1624
(2007/10/03)
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- The synthesis and applications of 5-aminolevulinic acid (ALA) derivatives in photodynamic therapy and photodiagnosis
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A route has been developed to high-purity precursors, viz., ALA esters, to be used in photodiagnosis and photodynamic therapy. Hexyl, butyl and methyl 5-aminolevulinates are similar to the ALA acid in chemical stability and efficacy in producing the appropriate photosensitizer PpIX. Tests carried out on animal models showed the method based on the esters to be the more selective.
- Dabrowski, Zbigniew,Kwasny, Miroslaw,Kaminski, Jaroslaw,Beldowicz, Maria,Lewicka, Lidia,Obukowicz, Bozena,Kaliszewski, Miron,Pirozynska, Ewa
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p. 219 - 224
(2007/10/03)
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- Reinvestigation of the sulfuric acid-catalysed cyclisation of brominated 2-alkyllevulinic acids to 3-alkyl-5-methylene-2(5H)-furanones
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A synthesis of ethyl-, butyl-, hexyl- and dodecyl-substituted fimbrolides from alkyl-substituted levulinic acid derivatives through bromination and acid promoted lactonisation is described. The underlying reactions have been investigated using levulinic acid as a model, and the effects of varying the bromination conditions and changing acid concentration on product distribution are discussed. Dibromination proceeds best in CHCl3 and proceeds in EtOH-free CHCl3 without the complication of ester formation. Cyclisation. occurs with concomitant oxidation in 98-100% H2SO4 but gives highest yields of fimbrolides in 100% H2SO4. The formation of related beckerelide substances is also described.
- Manny, Anthony J.,Kjelleberg, Staffan,Kumar, Naresh,De Nys, Rocky,Read, Roger W.,Steinberg, Peter
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p. 15813 - 15826
(2007/10/03)
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- α-methylene-5-thiazolacetic acid esters
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A compound of the formula STR1 wherein Ar is phenyl optionally substituted with at least one member of the group consisting of halogen, methylenedioxy, phenyl, phenoxy, --CF3 and alkyl, alkoxy and alkylthio of 1 to 6 carbon atoms, Z is selected from the group consisting of hydrogen, chlorine, --CF3 and alkyl, alkoxy and alkylthio of 1 to 6 carbon atoms, R1 and R2 are individually alkyl of 1 to 6 carbon atoms and the exocyclic double bonds independently have (E) or (Z) geometry having fungicidal activity and a process for their preparation.
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- α-Methylene-4-(phenoxymethyl)-5-thiazolacetate
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A compound of the formula STR1 wherein Ar is phenyl optionally substituted with at least one member of the group consisting of halogen, methylenedioxy, phenoxy, phenyl, --CF3 and alkyl, alkoxy and alkylthio of 1 to 6 carbon atoms, Z is selected from the group consisting of hydrogen, chlorine, --CF3 and alkyl, alkoxy and alkylthio of 1 to 6 carbon atoms, R1 and R2 are individually alkyl of 1 to 6 carbon atoms and the exocyclic double bond has (Z) or (E) configuration having fungicidal activity.
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