Iridium-catalyzed enantioselective intramolecular hydroarylation of allylic aryl ethers devoid of a directing group on the aryl group
Although intramolecular hydroarylation is an attractive transformation of allylic aryl ethers, it has suffered from narrow substrate scope. We herein describe Ir/(S)-DTBM-SEGPHOS-catalyzed intramolecular hydroarylation of allylic aryl ethers. The reaction
A (different) bright ammonia amide carbamate derivative and application thereof (by machine translation)
The invention belongs to the field of plant, relates to a general formula (I) is shown in a (different) bright ammonia amide carbamate derivatives and their pharmaceutically acceptable salt, wherein substituent R has the definition given in the specification, the invention also relates to the general formula (I) preparation of compounds of the, specifically for the preparation of the intermediate of its development and application of plant disease control. (by machine translation)
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Paragraph 0036; 0037; 0038; 0059; 0060
(2017/07/14)
Design, synthesis and effect of the introduction of a propargyloxy group on the fungicidal activities of 1-substituted phenoxypropan-2-amino valinamide carbamate derivatives
The cell walls of oomycetes are composed of cellulose, making cellulose synthase enzymes good targets for carboxylic acid amide fungicides. Valinamide carbamates are amino acid fungicides that represent excellent alternatives to conventional synthetic pesticides in terms of their ability to reduce the negative impacts of these compounds on human health and the environment. In a continuation of our research towards the development of new cellulose synthase inhibitors, we have developed a series of "stretched" analogues of iprovalicarb by the introduction of an additional OCH2 linker. The bioassay results indicated that compounds containing a small group at the para-position of phenyl gave excellent fungicidal activities with EC50 values ranging from 0.59 to 2.06 μmol L-1. Most notably, the introduction of a propargyloxy group led to a pronounced increase in the fungicidal activity. Furthermore, compound 7o bearing a propargyloxy group was identified as the most promising candidate because of its excellent fungicidal potency against oomycete diseases and good fungicidal activity against non-oomycete diseases.
Discovery of amino-acetonitrile derivatives, a new class of synthetic anthelmintic compounds
A new series of amino-acetonitrile derivatives (AAD) have been discovered that exhibit high anthelmintic activity against parasitic nematode species such as Haemonchus contortus and Trichostrongylus colubriformis. Significantly, these compounds also demonstrate activity against nematode strains resistant to the currently available broad-spectrum anthelmintics. The discovery, synthesis, structure-activity relationship and biological results are presented.