- Monodentate Transient Directing Group Enabled Pd-Catalyzed Ortho-C-H Methoxylation and Chlorination of Benzaldehydes
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We report Pd-catalyzed ortho-C-H methoxylation and chlorination of benzaldehydes by employing monodentate transient directing groups (TDGs) as an alternative strategy to bidentate TDGs. More importantly, a single crystal of benzaldehyde imine ortho-cyclopalladium intermediate was successfully obtained, and its structure was unambiguously determined by X-ray diffraction, which clearly showed that it was a binuclear palladium species bridged by a pyridone ligand. The utility of this approach was further demonstrated through the synthesis of key intermediates of natural products and drugs.
- Li, Feng,Zhou, Yirong,Yang, Heng,Wang, Ziqi,Yu, Qinqin,Zhang, Fang-Lin
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supporting information
p. 3692 - 3695
(2019/05/24)
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- DUAL-ACTING ANTIHYPERTENSIVE AGENTS
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In one aspect, the invention relates to compounds having the formula: wherein: Ar, r, Z, X, R3, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
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Page/Page column 42-43
(2010/02/17)
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- METHOD FOR THE PRODUCTION OF LOSARTAN
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The invention relates to a novel method for the production of losartan, an imidazol derivative with the chemical name 2-n-butyl-4-chloro-5-hydroxymethyl-1-{[2'-(1H-tetrazol-5-yl)biphenyl-4-]methyl}imidazol and the pharmacologically active salts thereof. The invention also relates to novel intermediate products which are suitable for the production of losartan, and to novel methods for the production of intermediate compounds which are suitable for the production of losartan. One aspect of the invention is a method for the production of a compound of general formula (I), which can arise as an intermediate step in the inventive representation of losartan.
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Page/Page column 16; 26-27
(2008/06/13)
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- Imidazolyl-propenoic acid derivatives
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Imidazolyl-propenoic acid derivatives can be prepared by reaction of aldehydes with phosphonoacetic acid esters. The imidazolyl-propenoic acid derivatives are suitable as active substances in medicaments, in particular in hypotensive and anti-atherosclero
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