- Synthesis of Cyclopropyl Ester and Amide Substituted Pyrimidinediones as Protoporphyrinogen Oxidase-Inhibiting Herbicides
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The protoporphyrinogen oxidase (PPO) enzyme is involved in the biosynthesis of chlorophyll and is an important target in research for development of new herbicides. In this study, new pyrimidinedione compounds with thioester tail group containing cyclopropyl moiety are synthesized from the commercially available 2-(1-(mercaptomethyl)cyclopropyl)acetic acid. The herbicidal activity of the synthesized compounds is also evaluated. Most of the synthesized compounds exhibit herbicidal activities against both monocot and dicot weeds. In particular, 10a showed similar activity to the control material, Saflufenacil. And when against the monocot weeds, Echinochloa crusgalli and Digitaria sanguinalis, 10a shows superior activity to Saflufenacil.
- Choi, Jong-Soo,Kwon, Young Bin,Lee, Kye Hwan,Lee, Won Hyung,Seu, Young-Bae
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p. 420 - 428
(2021/01/18)
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- Preparation method of 1-mercaptomethylcyclopropylacetic acid
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The invention relates to a preparation method of 1-mercaptomethylcyclopropylacetic acid, and belongs to the technical field of raw material preparation. The technical scheme comprises the steps: using 2,5-dimethyl-2,5-dihydroxy-1,4-dithiane described in a formula 1 as a starting material, preparing alpha,beta-unsaturated carboxylic acid ester shown in a formula 2 in an alkaline reagent environment, then adopting 1,2-dimethylimidazole as a basic catalyst, preparing beta,gamma-unsaturated carboxylic acid ester of a formula 3 under irradiation of ultraviolet light, then performing a Simmons-Smith reaction on the beta,gamma-unsaturated carboxylic acid ester of the formula 3 and diethylzinc and diiodomethane so as to obtain a cyclopropanation intermediate shown in a formula 4, and performing hydrolysis on the cyclopropanation intermediate of the formula 4 under an alkaline condition so as to obtain the target compound 1-mercaptomethylcyclopropylacetic acid. The defects of highly toxic products, easy combustion and easy explosion, a large amount of waste liquid and no environmental protection in the prior art are overcome.
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Paragraph 0019; 0028
(2019/10/04)
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- A PROCESS FOR PREPARATION OF MONTELUKAST SODIUM SALT
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The present invention relates to a process for the preparation of montelukast sodium salt. The process includes (a) reacting 2-(2-(3-(S)-(3-(7-chloro-2- quinolinyl)-ethenyl) phenyl)-3-hydroxypropyl)- phenyl-2-propanol of Formula (II) with diphenyl chloro phosphate to get a compound of Formula III; (b) condensing the compound of Formula III with a compound of Formula IV to get compound of Formula V; (c) and converting the compound of Formula V to montelukast sodium of Formula (I).
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Page/Page column 13
(2009/12/23)
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- IMPROVED PROCESS FOR PURE MONTELUKAST SODIUM THROUGH PURE INTERMEDIATES AS WELL AS NOVEL AMINE SALTS
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The present invention provides an improved process for the preparation of highly pure montelukast sodium through highly pure diol intermediate compound of formula (2) and (1)-(mercapto methyl) cyclopropane acetic acid methyl ester compound of formula (4) or mercaptomethyl cyclopropane acetic acid compound of formula (7). The present invention also provides novel organic amine salts of montelukast.
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Page/Page column 33
(2008/12/05)
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- Process for preparation of [1-(mercaptomethyl)cyclopropyl]acetic acid and related derivatives
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The present invention provides a novel process for preparing [1-(mercaptomethyl)cyclopropyl]acetic acid with high purity and related derivatives.
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Page/Page column 9
(2008/06/13)
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- NEW TRICYCLIC DERIVATIVES AS LTD4 ANTAGONISTS
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Compounds of formula (I) and their pharmaceutically acceptable salts are provided as well as processes for the manufacture of such compounds. The compounds are useful in the treatment or prevention of inflammatory and allergic diseases.
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- DIARYL 5,6-FUSED HETEROCYCLIC ACIDS AS LEUKOTRIENE ANTAGONISTS
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Compounds having the formula I: STR1 are antagonists of the actions of leukotrienes. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.
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- HETEROARYL AND HALOARYL QUINOLINE DERIVATIVES OF CYCLOPROPANEACETIC ACID AS LEUKOTRIENE ANTAGONISTS
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Compounds having the formula I: STR1 are antagonists of the actions of leukotrienes. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.
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