- Preparation method of metconazole (by machine translation)
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The method comprises the following steps: 2 - (2 - chlorobenzylidene) 2 - 2 -methylcyclopentanone and p-chlorobenzaldehyde react to obtain an epoxide; the epoxide reacts with triazole to obtain an epoxide; and the epoxide is reacted with triazole to obtain an open-loop product; and the ring-opening product 4 - is subjected -2 to 2 - catalytic hydrogenation to obtain the 2 - myclobutanil . 4 - beta-(4 -chlorbenzydrospirone; 5 -2 -5 -chlorobenzyl) 5 - and methylcyclopentanone react. Corey-Chayyyysky is obtained. The preparation method is low in cost, easy to obtain in the market; the reaction steps are all conventional reactions, reaction steps are simple, implementation; process is simple, reaction conditions are mild, operation; conversion rate is high, reaction time is short, control, and industrialization production. (by machine translation)
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- [...] and its preparation method (by machine translation)
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The invention discloses a high-purity [...] and its preparation method; its preparation as follows: cyclopentanone and P-formaldehyde condensation reaction to obtain the exocyclic double bond of the α, β - unsaturated ketone (II); then and methylation reagent reaction to obtain the α ', α' - double-methyl substituted exocyclic double bond of the α, β - unsaturated ketone (III); then under the action of catalyst and hydrogen reduction of the double bond is obtained by reaction of 2, 2 - dimethyl - 5 - (4 - benzylic) cyclopentanone (IV); the reduction product (IV) generating Johnson - Corey - Chaykovsky reaction to obtain the epoxy propane compound (V); finally the epoxy propane compounds (V) and 1, 2, 4 - triazole reaction and after recrystallized to obtain high-purity [...] (I). Preparation method of this invention the raw material is cheap, short route, good selectivity, high total yield, good atom economy advantages, is extremely suitable for industrial production. (by machine translation)
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Paragraph 0057; 0070; 0071
(2018/03/24)
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- New and convenient approach for synthesis of metconazole
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In terms of environmental and food supply protection, development of green, efficient, and less toxic pesticides is of great importance and in continuous demand. Metconazole, a triazole antiseptic, possesses such advantages, being environmentally friendly and high efficiency with broad-spectrum activity against bacteria and fungi. However, previously reported synthetic routes for metconazole have many disadvantages, for example, requiring multiple steps, being complicated, and suffering from high cost. We report herein a new, convenient, and high-yield four-step (aldol condensation, dimethylation, hydrogenation, and one-pot triazolation) synthesis for metconazole with relatively low cost.
- Chen, Shusheng,Zhou, Muxing,Zhang, Zhenfeng,Zhang, Wanbin
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p. 6293 - 6298
(2017/10/03)
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- Triticonazole a process for the preparation of intermediates
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The invention relates to a preparation method for a triticonazole intermediate 5-(4-chlorobenzylidene)-2,2-dimethylcyclopentanone. The preparation method comprises: (1) performing an oximation reaction on cyclopentanone and morpholine in an organic solvent in the presence of p-methylbenzene sulfonic acid at a temperature of 40-80 DEG C, so as to generate an intermediate I; (2) performing a condensation reaction on the intermediate I and p-chlorobenzaldehyde in a solvent at a temperature of 40-80 DEG C, so as to generate an intermediate II; (3) hydrolyzing the intermediate II under an acidic condition to generate an intermediate III; and (4) performing a methylation reaction on the intermediate III and a halogenated methane in a polar solvent in the presence of a strong base at a temperature of 40-80 DEG C, so as to generate 5-(4-chlorobenzylidene)-2,2-dimethylcyclopentanone. The technology is relatively simple, is capable of effectively controlling the impurity content in the product a improving the product impurity, and is low in cost and beneficial for realizing nationalization of triticonazole.
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Paragraph 0064; 0065
(2017/02/28)
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- Design, Synthesis, and Cytotoxicity of Novel 3-Arylidenones Derived from Alicyclic Ketones
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Forty-four novel chalcone-inspired analogs having a 3-aryl-2-propenoyl moiety derived from alicyclic ketones were designed, synthesized, and investigated for cytotoxicity against murine B16 and L1210 cancer cell lines. The analogs belong to four structurally divergent series, three of which (series g, h, and i) contain differently substituted cyclopentanone units and the fourth (series j) contains a 3,3-dimethyl-4-piperidinone moiety. Of these, the analogs in series j showed potential cytotoxic activity against murine B16 (melanoma) and L1210 (lymphoma) cells. The most active compounds 5j, 11j, 15j, and 12h produced IC50 values from 4.4 to 15μm against both cell lines. A single-crystal X-ray structure analysis and molecular modeling studies confirmed that these chalcones have an E-geometry about the alkene bond and possess a slightly 'twisted' conformation similar to that of combretastatin A-4. At a concentration of 30μm, compounds 5j, 11j, and 15j did not cause microtubule depolymerization in cells, suggesting that they have a different mechanism of action. Forty-four novel chalcone-inspired analogs were designed and synthesized. Several compounds gave IC50 values 4.4-15μm against the growth of L1210 and B16 murine cancer cells.
- Satam, Vijay,Bandi, Ravi K.,Behera, Ajaya K.,Mishra, Bijay K.,Tzou, Samuel,Brockway, Olivia,Babu, Balaji,Zeller, Matthias,Westbrook, Cara,Mooberry, Susan L.,Lee, Moses,Pati, Hari
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experimental part
p. 700 - 708
(2012/04/04)
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- Fungicidal compositions containing (benzylidene)-azolylmethylcycloalkane
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(Benzylidene)-azolylmethylcycloalkane or -alkene of formula STR1 in which: A and A1 are hydrocarbon chains of 1 to 3 carbon atoms, R1, R2, R3, R4 and R5 are hydrocarbon radicals, X is halog
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