ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTTricyclic quinuclidylidenes as potential antihistamine-bronchodilating agentsFrank J. Villani, Thomas A. Mann, and Elizabeth A. WeferCite this: J. Med. Chem. 1975, 18, 7, 666–669Publication Date (Print):July 1, 1975Publication History Published online1 May 2002Published inissue 1 July 1975https://pubs.acs.org/doi/10.1021/jm00241a004https://doi.org/10.1021/jm00241a004research-articleACS PublicationsRequest reuse permissionsArticle Views129Altmetric-Citations11LEARN 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

Aus den Oxo‐Verbindungen (I) erhält man mit 3‐Chlorchinuclidin (II) in Gegenwart von Na die Carbinole (III), aus (IV) erhält man über das Li‐Derivat mit 3‐Chinuclidon (V) die Carbinole (VI).

The preparation of the four isomeric azaxanthones 3 and a number of their aromatic ring substituted derivatives is described. These ketones were converted into the title compounds which were examined for their biological properties. The most interesting compound in this series, the 1-methyl-4-piperidylidene derivative of 1-azaxanthene, shows the profile of an orally effective potent bronchodilating agent as well as a moderate antihistamine. Biological properties of this compound were compared to a number of antihistamines as well as known bronchodilating agents. Structure-activity relationships are also discussed.

Abstract2‐Chlomicotinsäure (I) reagiert mit den Phenolen (II) zu den Phenoxy‐Verbindungen (III), aus 3‐Hydroxy‐4‐picolin (IV) und Brombenzol (V) entsteht das Phenoxy‐Derivat (VI), das zur Carbonsäure (VII) oxidiert wird.

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTBenzopyranopyridine derivatives. 2. Reaction of azaxanthones with hydroxylamineFrank J. Villani, Janet Hannon, Elizabeth A. Wefer, Thomas A. Mann, and James B. MortonCite this: J. Org. Chem. 1975, 40, 12, 1734–1737Publication Date (Print):June 1, 1975Publication History Published online1 May 2002Published inissue 1 June 1975https://doi.org/10.1021/jo00900a012Request reuse permissionsArticle Views245Altmetric-Citations11LEARN 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 InReddit PDF (512 KB) Get e-Alertsclose Get e-Alerts

Abstract3‐Cyan‐4‐picolin (I) liefert mit Benzaldehyd (II) das trans‐Kondensat (IIIa), das zu (IIIb) isomerisiert und dann zum Lactam (IV) cyclokondensiert wird.

AbstractDie Azaketone (I) mit einem Stickstoffatom in den Stellungen 1, 2, 3 oder 4 reagieren mit den Grignardreagentien (II) zu den Carbinolen (III), aus denen durch Dehydratisierung in Gegenwart von 85%iger Schwefelsäure oder Polyphosphorsäure die Olefine (IV) erhalten werden.

An improved synthesis of the title compound is described. The base catalyzed condensation of 4‐methylnicotinonitrile with benzaldehyde resulted in the isolation of trans ‐ 4 ‐styrylnicotin‐amide ( 2a ) in high yield. Hydrolysis to the acid and heating the acid 3a with polyphosphoric acid (ppa) gave the title compound 1a in good yields. Even higher yields of 1a were obtained in the presence of catalytic quantities of selenium. Also described are two other syntheses of the title compound as well as the preparation of a series of compounds related to 2a (Table I).

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTDerivatives of 10,11-dihydro-5H-dibenzo[a,d]cycloheptene and related compounds. 6. Aminoalkyl derivatives of the aza isosteresFrank J. Villani, Peter J. L. Daniels, Claire A. Ellis, Thomas A. Mann, Kai-Chih Wang, and Elizabeth A. WeferCite this: J. Med. Chem. 1972, 15, 7, 750–754Publication Date (Print):July 1, 1972Publication History Published online1 May 2002Published inissue 1 July 1972https://pubs.acs.org/doi/10.1021/jm00277a013https://doi.org/10.1021/jm00277a013research-articleACS PublicationsRequest reuse permissionsArticle Views448Altmetric-Citations27LEARN 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

Abstract3‐Chinuclidon‐hydrochlorid (I) liefert die Benzyliden‐Verbindung (II), die nach katalytischer Hydrierung zur Benzylverbindung (III) mit Triäthylphosphonoacetat zum Olefin (IV) kondensiert wird.

Journal of Heterocyclic ChemistryVolume 7, Issue 4 p. 973-974 Note Preparation of 3,4,4a,5,11,11a-Hexahydro-1,4-ethano-1H-benzo[5,6] cyclohepta-[1,2-b] pyridin-6-(2H)one Frank J. Villani, Frank J. Villani Department of Medicinal Chemistry, Schering Corporation, Bloomfield, New Jersey 07003Search for more papers by this authorElizabeth A. Wefer, Elizabeth A. Wefer Department of Medicinal Chemistry, Schering Corporation, Bloomfield, New Jersey 07003Search for more papers by this author Frank J. Villani, Frank J. Villani Department of Medicinal Chemistry, Schering Corporation, Bloomfield, New Jersey 07003Search for more papers by this authorElizabeth A. Wefer, Elizabeth A. Wefer Department of Medicinal Chemistry, Schering Corporation, Bloomfield, New Jersey 07003Search for more papers by this author First published: August 1970 https://doi.org/10.1002/jhet.5570070443Citations: 1AboutPDF ToolsRequest permissionExport citationAdd to favoritesTrack citation ShareShare Give accessShare full text accessShare full-text accessPlease review our Terms and Conditions of Use and check box below to share full-text version of article.I have read and accept the Wiley Online Library Terms and Conditions of UseShareable LinkUse the link below to share a full-text version of this article with your friends and colleagues. Learn more.Copy URL No abstract is available for this article.Citing Literature Volume7, Issue4August 1970Pages 973-974 RelatedInformation

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTDerivatives of 2-azabicyclo[2.2.2]octane. III. Substituted phenylsulfonylureido derivativesFrank J. Villani, Elizabeth A. Wefer, Thomas A. Mann, and Claire A. EllisCite this: J. Med. Chem. 1969, 12, 5, 933–934Publication Date (Print):September 1, 1969Publication History Published online1 May 2002Published inissue 1 September 1969https://pubs.acs.org/doi/10.1021/jm00305a060https://doi.org/10.1021/jm00305a060research-articleACS PublicationsRequest reuse permissionsArticle Views48Altmetric-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