A series of N-alkyl-N-arylmethylpiperidin-4-amines have been prepared and are demonstrated to be inhibitors of both serotonin and norepinephrine reuptake.

Two routes to the protected 4-hydroxymethyl-3-methylindole-2-carboxylate fragment 17 of the thiopeptide antibiotic nosiheptide are described starting from methyl 4-methylindole-2-carboxylate 11, itself prepared in two steps, or from 3-amino-4-chlorobenzoic acid 26. The first route can be adapted to the synthesis of a fragment of the related antibiotic glycothiohexide-alpha, the 3,4-bis(hydroxymethyl)indole-2-carboxylate in which the two hydroxymethyl groups are differentiated as in indole 19 or the lactone 20.

A series of benzothienyloxy propylamines have been prepared and are demonstrated to be inhibitors of both serotonin and norepinephrine reuptake.

The University of Huddersfield is the only institution to have been validated by the CPE Board to deliver the Postgraduate Diploma in Law (Common Professional Examination) course for delivery by distance learning, using the Internet as the principal method of delivery. The course came on-stream for the 1998/99 academic year. The previous JILT article in October 1999, consisted of a detailed evaluation of the course following its first year of delivery. This is a follow-up article consisting of an evaluation of the course following the conclusion of the 1999/2000 academic year. It is more comprehensive given the fact there were students on both years of the course, and July 2000 witnessed the first graduates. The article offers an insight into the future of electronically delivered law courses at both postgraduate and undergraduate level.

4′-N-desmethyl olanzapine (2), olanzapine 4′-N-oxide (3) and 2-hydroxymethyl olanzapine (5), have been prepared and their pharmacology compared to that of the parent compound olanzapine (1). The 4′-N-quaternary glucuronide (8) has also been prepared.

A series of 2-thioether derivatives of a number of clavine alkaloid (ergoline) ring systems have been synthesized and tested for dopamine antagonist activity. Of the compounds tested 2-(methylthio)-agroclavine (8,9-didehydro-6,8-dimethyl-2-(methylthio)ergoline) (6) was the most potent and had a profile of activity in animal models indicative of potential antipsychotic activity. The synthesis and biological activity of a number of metabolites of 6, including the 13-hydroxy derivative, are also reported.

Chemischer InformationsdienstVolume 12, Issue 5 Heterocyclic Compounds ChemInform Abstract: HETEROARENOBENZODIAZEPINES. 4. 10-PIPERAZINYL-4H-THIENO(3,2-B)(1,5)- AND -(3,4-B)(1,5)BENZODIAZEPINES AS POTENTIAL NEUROLEPTICS J. K. CHAKRABARTI, J. K. CHAKRABARTISearch for more papers by this authorJ. FAIRHURST, J. FAIRHURSTSearch for more papers by this authorN. J. A. GUTTERIDGE, N. J. A. GUTTERIDGESearch for more papers by this authorL. HORSMAN, L. HORSMANSearch for more papers by this authorI. A. PULLAR, I. A. PULLARSearch for more papers by this authorC. W. SMITH, C. W. SMITHSearch for more papers by this authorD. J. STEGGLES, D. J. STEGGLESSearch for more papers by this authorD. E. TUPPER, D. E. TUPPERSearch for more papers by this authorF. C. WRIGHT, F. C. WRIGHTSearch for more papers by this author J. K. CHAKRABARTI, J. K. CHAKRABARTISearch for more papers by this authorJ. FAIRHURST, J. FAIRHURSTSearch for more papers by this authorN. J. A. GUTTERIDGE, N. J. A. GUTTERIDGESearch for more papers by this authorL. HORSMAN, L. HORSMANSearch for more papers by this authorI. A. PULLAR, I. A. PULLARSearch for more papers by this authorC. W. SMITH, C. W. SMITHSearch for more papers by this authorD. J. STEGGLES, D. J. STEGGLESSearch for more papers by this authorD. E. TUPPER, D. E. TUPPERSearch for more papers by this authorF. C. WRIGHT, F. C. WRIGHTSearch for more papers by this author First published: February 3, 1981 https://doi.org/10.1002/chin.198105261Read the full textAboutPDF 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 Share a linkShare onFacebookTwitterLinked InRedditWechat No abstract is available for this article. Volume12, Issue5February 3, 1981 RelatedInformation

The synthesis of 10-piperazinyl-4H-thieno[3,2-b][1,5]benzodiazepines is described. The activity of these compounds has been assessed on the basis of their ability to produce hypothermia in mice and block a conditioned avoidance response (CAR) and produce catalepsy in rats, and the results are compared with various classical and nonclassical neuroleptic drugs. A number of compounds (6, 17, 21, and 22) demonstrate potency greater than clozapine and also show low degree of catalepsy. It is believed that this profile of activity, unlike standard neuroleptics, is associated with the relative lack of extrapyramidal side effects in the clinic. The corresponding 9-piperazinyl-4H-thieno[1,4]benzodiazepines (12 and 35, limited analogues prepared in the respective series, were inactive.

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTHeteroarenobenzodiazepines. 4. 10-Piperazinyl-4H-thieno[3,2-b][1,5]- and -[3,4-b][1,5]benzodiazepines as potential neurolepticsJiban K. Chakrabarti, John Fairhurst, Norman J. A. Gutteridge, Linda Horsman, Ian A. Pullar, Colin W. Smith, David J. Steggles, David E. Tupper, and Francesca C. WrightCite this: J. Med. Chem. 1980, 23, 8, 884–889Publication Date (Print):August 1, 1980Publication History Published online1 May 2002Published inissue 1 August 1980https://pubs.acs.org/doi/10.1021/jm00182a014https://doi.org/10.1021/jm00182a014research-articleACS PublicationsRequest reuse permissionsArticle Views447Altmetric-Citations23LEARN 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

AbstractAus dem Cyclohexadien (I) und den isomeren Nitrilen (IIa) bzw. (IIb) werden die Cyanbicyclooctane (IIIa) bzw. (IIIb) synthetisiert, deren Reduktionsprodukte (IVa) bzw. (IVb) zu den Dimethylaminoderivaten (Va) bzw. (Vb) umgesetzt RI werden; die analog (IV) synthetisierten Aminomethylbicyclooctane (VI) werden nach einer modifizierten Eschweiler‐Clarke‐Methode zu den Derivaten (VII) N,N‐dimethyliert Die trans‐Diels‐Alder4Addukte (IX) ‐ zugänglich aus (I) und den trans‐Zimtaldehyden (VIII) ‐ werden durch Bromierung/Dehydrobromierung in die ungesättigten Aldehyde (X) übergeführt; Kondensation der Aldehyde (X) mit Methylamin gibt die entsprechenden Imine, die zu den sek. Aminen (XI) reduziert werden; diese lassen sich analog (VI) zu den tertiären Aminen (XII) umsetzen.

AbstractCyclohexadien (I) reagiert mit 2‐Chlor‐ 3‐nitro‐propionsäureester (II) zu den stereoisomeren Addukten (III) und (IV).

AbstractThe synthesis of the novel bicyclo[2.2.2]octanyl[1,4]benzodiazepinone ring system (IV) and its facile acid catalysed rearrangement to the corresponding bicyclo[2.2.2]oct‐2‐enylbenzirnid‐azole system (IX) is described.

Chemischer InformationsdienstVolume 7, Issue 30 Preparative Organic Chemistry ChemInform Abstract: A CONVENIENT PROCEDURE FOR ESTERIFICATION OF THERMALLY UNSTABLE CARBOXYLIC ACIDS J. FAIRHURST, J. FAIRHURSTSearch for more papers by this authorD. C. HORWELL, D. C. HORWELLSearch for more papers by this author J. FAIRHURST, J. FAIRHURSTSearch for more papers by this authorD. C. HORWELL, D. C. HORWELLSearch for more papers by this author First published: July 27, 1976 https://doi.org/10.1002/chin.197630141Read the full textAboutPDF 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 Share a linkShare onFacebookTwitterLinked InRedditWechat No abstract is available for this article. Volume7, Issue30July 27, 1976 RelatedInformation

There are many new methods for esterifying carboxylic acids but some have specific limitations such as harsh conditions, inconvenience of procedure, expense and inaccessibility of reagents1-6 we have prepared several novel bicyclic β–keto acids as intermediates for the synthesis of heterocyclic systems. Since these β–keto acids readily decarboxylate on heating, esterification by a simple low temperature procedure was necessary.

AbstractAus den Aldehyden (I) und Cyanessigsäure (II) entstehen die Kondensate (III), die in Gegenwart von Kupferoxid/Benzol zu den ungesättigten Nitrilen (IV) decarboxyliert werden können.