Polarized ethylenes. IV. Synthesis of polarized ethylenes using thioamides and methyl dithiocarboxylates and their application to syntheses of pyrazoles, pyrimidines, pyrazolo[3,4‐d]pyrimidines, and 5‐aza[2.2.3]cyclazines
TL;DR: Polarized ethylenes having both electron-donating (an amino or a methylthio group) and electron-accepting (cyano, carbamoyl, methyl ester) groups on the adjacent two olefinic carbon atoms were prepared by the condensation of S-alkylthioamidinium salts or methyl dithiocarboxylates with the corresponding active methylene compounds in good yields.
About: This article is published in Journal of Heterocyclic Chemistry.The article was published on 1990-03-01. It has received 59 citations till now. The article focuses on the topics: Pyrazole & Tetracyanoethylene.
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TL;DR: The src-family protein kinase inhibitors as mentioned in this paper are selective inhibitors of protein kinases, and are of use in the prophylaxis and treatment of immune diseases, hyperproliferative disorders and other diseases in which inappropriate kinase action is believed to have a role.
Abstract: Compounds of formula (1) are described and the salts, solvates, hydrates and N-oxides thereof, in which R?1, R2, R3, R4, R5, R6 and R7? have the meanings given in Claim 1. The compounds are selective inhibitors of protein kinases, especially src-family protein kinases and are of use in the prophylaxis and treatment of immune diseases, hyperproliferative disorders and other diseases in which inappropriate protein kinase action is believed to have a role.
300 citations
155 citations
Patent•
19 Jun 2000
TL;DR: Pyrimidines of formula (1) are described wherein Ar is an optionally substituted aromatic or heteroaromatic group; R 1 is a hydrogen atom or a straight or branched chain alkyl group, R 2 is a -X1-R3 group where X1 is a direct bond or a linker atom or group.
Abstract: Pyrimidines of formula (1) are described wherein Ar is an optionally substituted aromatic or heteroaromatic group; R1 is a hydrogen atom or a straight or branched chain alkyl group; R2 is a -X1-R3 group where X1 is a direct bond or a linker atom or group, and R3 is an optionally substituted aliphatic, cycloaliphatic, heteroaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are selective KDR Kinase and/or FGFr Kinase inhibitors and are of use in the prophylaxis and treatment of disease states associated with angiogenesis.
117 citations
Patent•
22 Oct 1993
TL;DR: In this article, selective phosphodiesterase IV inhibitors were proposed for the prophylaxis or treatment of inflammatory diseases, and they were used for the treatment of various inflammatory diseases.
Abstract: Compounds are described in formula (1), wherein Y is a halogen atom or a group -OR1, where R1 is an optionally substituted alkyl group; R2 is an optionally substituted cycloalkyl or cycloalkenyl group; R3 is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, nitrogen or sulphur atoms or a group -N(R4)- where R4 is a hydrogen atom or an alkyl group; X is -O-, -S-, or -N(R5)-, where R5 is a hydrogen atom or an alkyl group; with the proviso that when X is -O- the R3 is not a 3-cyanamino-6-pyridazinyl or a 3-chloro-6-pyridazinyl group; and the salts, solvates, hydrates and N- oxides thereof. The compounds are selective phosphodiesterase IV inhibitors and are useful for the prophylaxis or treatment of inflammatory diseases.
109 citations
TL;DR: Protein Kinase Inhibitors: An Old Scaffold As a New Tool for Medicinal Chemistry and Chemical Biology Studies
Abstract: Protein Kinase Inhibitors: An Old Scaffold As a New Tool for Medicinal Chemistry and Chemical Biology Studies Silvia Schenone,*,† Marco Radi,‡ Francesca Musumeci,† Chiara Brullo,† and Maurizio Botta †Dipartimento di Farmacia, Universita ̀ degli Studi di Genova Viale Benedetto XV, 3, 16132 Genova, Italy ‡Dipartimento di Farmacia, Universita ̀ degli Studi di Parma Viale delle Scienze, 27/A, 43124 Parma, Italy Dipartimento di Biotecnologie, Chimica e Farmacia, Universita ̀ degli Studi di Siena Via Aldo Moro, 2, 53100 Siena, Italy Sbarro Institute for Cancer Research and Molecular Medicine, Center for Biotechnology, College of Science and Technology, Temple University, BioLife Science Building, Suite 333, 1900 N 12th Street, Philadelphia, Pennsylvania 19122, United States
105 citations
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299 citations
TL;DR: In this article, it was shown that sulfide contraction via alkylative coupling (see scheme p. 729) is a potentially general method for the synthesis of secondary vinylogous amides and enolizable β-dicarbonyl compounds.
Abstract: The experiments described in reaction schemes 1–12 indicate that sulfide contraction via alkylative coupling (see scheme p. 729) is a potentially general method for the synthesis of secondary vinylogous amides and enolizable β-dicarbonyl compounds.
256 citations
241 citations
TL;DR: In this paper, the herstellung von Dithiocarbonsauren aus CH-aciden Verbindungen und Schwefelkohlenstoff wird beschrieben.
Abstract: Die Herstellung von Dithiocarbonsauren aus CH-aciden Verbindungen und Schwefelkohlenstoff wird beschrieben. Die Alkylierung ihrer Salze fuhrt zu substituierten Ketenmercaptalen; bei der Oxydation entstehen Trithiacyclopentane und Dithiacyclobutane (Desaurine), letzter auch bei der Acylierung. Die Umsetzung mit Athylenimin liefert Thiazolidine. Die Struktur (Tautomerie) der Dithiocarbonsaureester und Ketenmercaptale wird an Hand der IR-Spektren diskutiert.
190 citations
TL;DR: In this article, the Struktur des Benzoyl-dithioessaure-methylesters wird diskutiert und seine Umsetzung with Aminen beschrieben.
Abstract: Nitroketen-mercaptale (2, 4),-S.N-acetale (6) und -aminale (3) lassen sich aus Nitroalkanen herstellen. – Die Struktur des Benzoyl-dithioessigsaure-methylesters (9) wird diskutiert und seine Umsetzung mit Aminen beschrieben. – Aus Benzylcyanid, CS2/Alkali und Chloracet-amid entsteht 2-[Phenyl-cyan-methylen]-1.3-dithiolanon-(4) (18), das mit Aldehyden zu Cyaninfarbstoffen (20) reagiert. – Dithiocarbonsaureester vermogen sich an Chinone unter Bildung von 5-Hydroxy-benzo- und -naphtho-1.3-oxathiolen (23) zu addieren.
170 citations