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Showing papers by "Edward C. Taylor published in 1977"








Journal ArticleDOI
TL;DR: In this article, a non-phenolic coupling with thallium tris(trifluoroacetate) tris (TTFA) was proposed to synthesize Ocoteine, aporphine and 5,7-dihydro-2,3,9,10-tetramethoxydibenzo[c,e]oxepin.
Abstract: (±)-Ocoteine (8), the acetoxy aporphine (9), and 5,7-dihydro-2,3,9,10-tetramethoxydibenzo[c,e]oxepin (5) have been synthesized by direct non-phenolic coupling with thallium tris(trifluoroacetate)(TTFA).

12 citations


Journal ArticleDOI
TL;DR: Activity was found to depend upon ring size, with the greatest activity exhibited by the cyclododeca derivatives of 2,4,5,6-tetraaminopyrimidine.
Abstract: A number of homologous 2,4-diaminocycloalka[g]pteridines varying in ring size from 5 to 15 were prepared by (a) condensation of aminomalononitrile tosylate with alpha-oximinocycloalkanones, deoxygenation of the resulting 2-amino-3-cyanocycloalka[b]pyrazine 1-oxides, and guanidine cyclization; (b) guanidine cyclization of the above pyrazine 1-oxides to give 2,4-diaminocycloalka[g]pteridine 8-oxides, followed by deoxygenation; or (c) condensation of 2,4,5,6-tetraaminopyrimidine with a cycloalka-1,2-dione (for the cyclohepta- and cycloocta[g]pteridines only). These compounds were examined for their activity as dihydrofolate reductase inhibitors against Lactobacillus casei, rat liver, L1210, and Trypanosoma cruzi. Activity was found to depend upon ring size, with the greatest activity exhibited by the cyclododeca derivatives 31.

12 citations



Patent
26 Aug 1977
TL;DR: Improved supported thallium(III) reagents are provided in this article, which significantly improve reaction rates and product selectivity of oxythallation reactions, and have been shown to improve the performance of oxithallation.
Abstract: Improved supported thallium(III) reagents are provided which significantly improve reaction rates and product selectivity of oxythallation reactions. The present reagents have a thallium(III) salt of an acid on the surface and within montmorillonite clay minerals.

4 citations



Journal ArticleDOI
TL;DR: A number of homologous 2,4-diaminocycloalka[g]pteridines varying in ring size from 5 to 15 were prepared by condensation of aminomalononitrile tosylate with alpha-oximinocyCLoalkanones, deoxygenation of the resulting 2-amino-3-cyanocycloencysa[b]pyrazine 1-oxides, and guanidine cyclization;
Abstract: A number of homologous 2,4-diaminocycloalka[g]pteridines varying in ring size from 5 to 15 were prepared by (a) condensation of aminomalononitrile tosylate with alpha-oximinocycloalkanones, deoxygenation of the resulting 2-amino-3-cyanocycloalka[b]pyrazine 1-oxides, and guanidine cyclization; (b) guanidine cyclization of the above pyrazine 1-oxides to give 2,4-diaminocycloalka[g]pteridine 8-oxides, followed by deoxygenation; or (c) condensation of 2,4,5,6-tetraaminopyrimidine with a cycloalka-1,2-dione (for the cyclohepta- and cycloocta[g]pteridines only). These compounds were examined for their activity as dihydrofolate reductase inhibitors against Lactobacillus casei, rat liver, L1210, and Trypanosoma cruzi. Activity was found to depend upon ring size, with the greatest activity exhibited by the cyclododeca derivatives 31.


Patent
30 Sep 1977
TL;DR: Improved supported thallium(III) reagents are provided in this article, which significantly improve reaction rates and product selectivity of oxythallation reactions, and have been shown to improve the performance of oxithallation.
Abstract: Improved supported thallium(III) reagents are provided which significantly improve reaction rates and product selectivity of oxythallation reactions. The present reagents have a thallium(III) salt of an acid on the surface and within montmorillonite clay minerals.