Abstract The linearly coordinated title complex (I) was prepared by an improved route through reduction of chloroauric acid in H 2 O with thiodiglycol in MeOH (15 min, 0 °C) followed by addition of the diphosphine in CHCl 3 /MeOH.
Aus dem Dimethoxy-benzazepin (Ia) entsteht das Carbethoxy-Derivat (Ib), das mit Phenylsulfenylchlorid zu (IIa) substituiert und dann zu (IIb) reduziert wird.
Abstract Die Isochinoline (I) werden durch katalytische Hydrierung oder mit überschüssigem Diboran in Tetrahydrofuran zu den Tetrahydroisochinolinen (II) reduziert.
Cristallisation dans P2 1 /n avec Z=4; affinement jusqu'a R=0,031. Coordination plan carre. Observation d'un allongement appreciable de la liaison Au−Br trans par rapport a la phosphine, avec une longueur de liaison An−P normale. Les molecules sont monomeres et il n'y a pas de distances intermoleculaires inhabituellement courtes
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTNew synthesis of some arylthio-substituted 2,3,4,5-tetrahydro-1H-3-benzazepinesThomas W. Ku, Mary E. McCarthy, William E. Bondinell, Penelope A. Dandridge, Gerald R. Girard, and Carl KaiserCite this: J. Org. Chem. 1982, 47, 20, 3862–3865Publication Date (Print):September 1, 1982Publication History Published online1 May 2002Published inissue 1 September 1982https://pubs.acs.org/doi/10.1021/jo00141a011https://doi.org/10.1021/jo00141a011research-articleACS PublicationsRequest reuse permissionsArticle Views94Altmetric-Citations1LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InRedditEmail Other access optionsGet e-Alertsclose Get e-Alerts
A series of novel nonpeptide angiotensin II receptor antagonists containing a substituted (E)-acrylic acid has been developed. The overlay of 1, an imidazole-5-acetic acid found in the patent literature, on a novel pharmacophore model of AII suggested that extension of the acid side chain and attachment of a second aryl residue to mimic the C-terminal phenylalanine region of AII would lead to increased activity. A study of extended acid side chains at C-5 of the imidazole nucleus led to the discovery of the (E)-acrylic acid 5 as a promising starting point for further exploration. As predicted by the modeling, substitution of a benzyl group on the acrylic acid side chain to mimic the phenylalanine gave increased potency. An extensive study of the SAR of the newly introduced aromatic ring revealed that electron-rich heteroaryl rings provided improved activity, most notably in the in vivo rat models. Compound 40, (E)-3-[2-butyl-1- [(2-chlorophenyl)methyl]imidazol-5-yl]-2-[(2-thienyl)methyl]-2- propenoic acid, has been shown to be a potent, competitive, and orally active small molecule AT-1 receptor antagonist. It exhibits a 2 orders of magnitude increase in binding affinity and a 10-fold improvement in in vivo potency as compared to compound 1 and represents an important milestone in the development of even more potent nonpeptide angiotensin II receptor antagonists.
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXT[.mu.-1,1'-Bis(diphenylphosphino)ferrocene]bis(chlorogold): synthesis, iron-57 and gold-197 Moessbauer spectroscopy, x-ray crystal structure, and antitumor activityDavid T. Hill, Gerald R. Girard, Francis L. McCabe, Randall K. Johnson, Paul D. Stupik, Jian H. Zhang, William M. Reiff, and Drake S. EgglestonCite this: Inorg. Chem. 1989, 28, 18, 3529–3533Publication Date (Print):September 1, 1989Publication History Published online1 May 2002Published inissue 1 September 1989https://pubs.acs.org/doi/10.1021/ic00317a027https://doi.org/10.1021/ic00317a027research-articleACS PublicationsRequest reuse permissionsArticle Views639Altmetric-Citations129LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InRedditEmail Other access optionsGet e-AlertscloseSupporting Info (1)»Supporting Information Supporting Information Get e-Alerts
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