Total Synthesis of Anmindenol A and Its Application to the Design, Synthesis, and Biological Evaluation of Derivatives Thereof
The first total synthesis of anmindenol A is described in four steps. A notable feature of the synthetic route includes the efficient construction of the 3,10-dialkylsubstituted benzofulvene core via a stereoselective vinylogous Stork enamine aldol condensation. The strategy provided a blueprint for the practical preparation of derivatives with modifications in the C-10 alkyl substituents. The novel derivatives inhibited nitric oxide production in stimulated RAW 264.7 macrophage cells.
Jo, Jeyun,Jeong, Myeonggyo,Ahn, Ji-Su,Akter, Jinia,Kim, Hyung-Sik,Suh, Young-Ger,Yun, Hwayoung
New Synthetic Method of 3,10-disubstituted benzofulvene derivatives
The present invention relates to a novel synthesis method of 3,10-disubstituted benzofulvene derivatives which is excellent in an economic aspect since the yield is excellent. The novel synthesis method comprises the steps of: synthesizing an indene derivative having an enamine substituent; synthesizing an intermediate compound represented by chemical formula A; synthesizing an intermediate compound represented by chemical formula B; and synthesizing a 3,10-disubstituted benzofulvene derivative represented by chemical formula 3.COPYRIGHT KIPO 2020
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Paragraph 0070; 0108-0111
(2020/01/07)
Silylative Kinetic Resolution of Racemic 1-Indanol Derivatives Catalyzed by Chiral Guanidine
Efficient kinetic resolution of racemic 1-indanol derivatives was achieved using triphenylchlorosilane by asymmetric silylation in the presence of chiral guanidine catalysts. The chiral guanidine catalyst (R,R)-N-(1-(β-naphthyl)ethyl)benzoguanidine was found to be highly efficient as only 0.5 mol % catalyst loading was sufficient to catalyze the reaction of various substrates with appropriate conversion and high s-values (up to 89). This catalyst system was successfully applied to the gram-scale silylative kinetic resolution of racemic 1-indanol with high selectivity.
Yoshimatsu, Shuhei,Yamada, Akira,Nakata, Kenya
p. 452 - 458
(2018/02/19)
BICYCLICALLY SUBSTITUTED URACILS AND THE USE THEREOF
The present application relates to novel bicyclically substituted uracil derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases.
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Paragraph 0903; 0914; 0915; 0916; 0917
(2015/06/03)
SUBSTITUTED FLUOROETHYL UREAS AS ALPHA 2 ADRENERGIC AGENTS
Therapeutic compounds, and methods, compositions, and medicaments related thereto are disclosed herein.
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Page/Page column 16
(2008/12/04)
Catalytic enantioselective Negishi reactions of racemic secondary benzylic halides
This report describes the first enantioselective cross-couplings of racemic secondary benzylic halides, specifically, nickel-catalyzed Negishi reactions of bromides and chlorides. The catalyst components are commercially available and air-stable, and the reaction is not highly oxygen- or moisture-sensitive (it can be set up in the air). The method has been applied to the catalytic enantioselective synthesis of intermediates employed by others in the generation of bioactive compounds (e.g., trikentrin A and an androgen receptor agonist). Copyright
Arp, Forrest O.,Fu, Gregory C.
p. 10482 - 10483
(2007/10/03)
Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/- indanes and structurally modified derivatives: Potent and selective inhibitors of aldosterone synthase
Elevated aldosterone levels are key effectors for the development and progression of congestive heart failure and myocardial fibrosis. Recently, we proposed inhibition of aldosterone synthase (CYP11B2) as an innovative strategy for the treatment of these
Ulmschneider, Sarah,Müller-Vieira, Ursula,Klein, Christian D.,Antes, Iris,Lengauer, Thomas,Hartmann, Rolf W.
p. 1563 - 1575
(2007/10/03)
C-GLYCOSIDE DERIVATIVES AND SALTS THEREOF
The present invention provides C-glycoside derivatives and salts thereof, wherein B ring is bonded to A ring via -X- and A ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes related diseases such as an insulin-resistant diseases and obesity.
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Page/Page column 18
(2008/06/13)
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