- PROCESSES FOR THE PREPARATION OF FUNGICIDAL COMPOUNDS
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Provided herein are processes for the preparation of stereomerically enriched compounds of Formulas I-014, I-020, I-064, I-074, I-082, I-089, I-090, I-095, I-171, I-181, I-184, I-186, I-189, I-191, I-192, I-193, I-205, I-206, I-208, I-211, I-212, I-213, I-220, I-229, I-231, I-233, I-234, I-246, I-251, I-258, I-259, I-262, I-263, I-285, I-323 and I-400. The compounds described herein exhibit activity as pesticides and are useful, for example, in methods for the control of fungal pathogens and diseases caused by fungal pathogens in plants. A preferred process is directed to preparing a stereomerically enriched compound of Formula V-1 or V-2-F by assymetrical reduction in the presence of a chiral organometallic catalyst.
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Paragraph 00217
(2018/09/21)
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- Design, synthesis and biological evaluation of novel ring-opened cromakalim analogues with relaxant effects on vascular and respiratory smooth muscles and as stimulators of elastin synthesis
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Two new series of ring-opened analogues of cromakalim bearing sulfonylurea moieties (series A: with N-unmethylated sulfonylureas, series B: with N-methylated sulfonylureas) were synthesized and tested as relaxants of vascular and respiratory smooth muscle
- Bouhedja, Mourad,Peres, Basile,Fhayli, Wassim,Ghandour, Zeinab,Boumendjel, Ahcène,Faury, Gilles,Khelili, Smail
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p. 774 - 796
(2018/01/05)
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- Chromenones as potent bradykinin B1 antagonists
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A series of fused 6,6-bicyclic chromenones was investigated for activity against the bradykinin B1 receptor. SAR studies based on a pharmacophore model revealed compounds with high affinity for both human and rabbit B1. These compounds demonstrated favorable pharmacokinetic properties and 5-chlorochromenone 15 was efficacious in a carrageenan-induced mechanical hyperalgesia model for chronic pain.
- Bryan, Marian C.,Biswas, Kaustav,Peterkin, Tanya A.N.,Rzasa, Robert M.,Arik, Leyla,Lehto, Sonya G.,Sun, Hong,Hsieh, Feng-Yin,Xu, Cen,Fremeau, Robert T.,Allen, Jennifer R.
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scheme or table
p. 619 - 622
(2012/02/04)
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- Rate of Enolate Formation Is Not Very Sensitive to the Hydrogen Bonding Ability of Donors to Carboxyl Oxygen Lone Pair Acceptors; A Ramification of the Principle of Non-Perfect Synchronization for General-Base-Catalyzed Enolate Formation
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Two series of structures (1 and 2) possessing intramolecular hydrogen bonds to the lone-pair electrons of carbonyl oxygens have been examined to reveal the influence of the pKa of the hydrogen-bond donor on the rate of general-base-catalyzed enolate formation. The geometry of the hydrogen bonds is well accepted to be appropriate for intramolecular hydrogen-bond formation. Yet, as revealed by Bronsted plots, both series show very little dependence of the rate of enolate formation on the hydrogen-bond donor ability. The intramolecular hydrogen bonds give rate enhancements only on the order of 10-100-fold, and corrected Bronsted α-values are slightly below 0.1. The results can be understood by interpreting them in light of the Principle of Non-Perfect Synchronization. The results are consistent with the proton transfer occurring through an asynchronous transition state with the developing negative charge localized on carbon. We postulate that catalysts of enolate formation will be most effective if the binding groups are focused on stabilizing negative charge that is forming on the enolate carbon rather than on the enolate oxygen.
- Zhong, Zhenlin,Snowden, Timothy S.,Best, Michael D.,Anslyn, Eric V.
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p. 3488 - 3495
(2007/10/03)
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- Solvent directing immediate fluorination of aromatic ketones using 1- fluoro-4-hydroxy-1,4-diazoniabicyclo[2.2.2]octane bis(tetrafluoroborate)
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Reactions of aryl alkyl ketones with 1-fluoro-4-hydroxy1,4- diazoniabicyclo[2.2.2]octane bis(tetrafluoroborate) (Accufluor(TM) NFTh) in methanol result in selective and almost quantitative formation of the corresponding α-fluoroketones, while in acetonitrile exclusive fluorofunctionalisation of the activated aromatic ring take place.
- Stavber, Stojan,Jereb, Marjan,Zupan, Marko
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p. 1323 - 1324
(2007/10/03)
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- Process for killing internal helminths using certain 1,1-bis-(2-substituted-3-nitrophenyl)alkane or alkylene derivatives
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A method for killing internal parasites of warm blooded animals by treating the animals with an effective amount of a composition comprising a bis-(2-hydroxy-3-nitrophenyl)methane derivative; and novel bis(2-hydroxy-3-nitrophenyl)methane derivatives.
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