- Microwave-promoted syntheses of fluoren-9-ones and benzisoxazoles
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Synthesis of some new fluoren-9-ones and benzisoxazoles under both thermal and microwave conditions is reported. The prepared products under microwave conditions are obtained with high yields and within shorter reaction times. Reaction of lithiated bromobenzene with aromatic aldehydes 2a,b delivered diarylmethanols 3a,b that were oxidized to 4a,b. Compound 4a was cyclized to give methoxyfluoren-9-one 5, which was demethylated affording hydroxyfluoren-9-one 6. Compound 4b was reacted with triethyl phosphite to produce benzisoxazole 10. On the other hand, reaction of triethyl phosphite with 13a,b afforded a mixture of phosphoramidates 14a,b and benzisoxazoles 15a,b. The structures of the synthesized compounds have been elucidated unambiguously by NMR-spectroscopic methods including HH COSY, HSQC, and HMBC experiments.
- Haggam, Reda A.,El-Sayed, Hassan A.
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- Pharmaceutical compounds
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Pharmaceutical compounds of the formula STR1 in which R1 and R2 are each hydrogen, hydroxyl, halo, C1-4 alkyl, C1-4 alkoxy, acyloxy, --O-glucoside, optionally substituted phenyl or optionally substituted phenyl-C1-4 alkoxy; R3 is tetrazolyl, or and R4 and R5 are each hydrogen, hydroxy, acyloxy, nitro, C1-4 alkyl, C1-4 alkoxy, halo, optionally substituted phenyl, --SO3 H or --NR'R" where R' and R" are each hydrogen or C1-4 alkyl; provided that when R3 is --CR'R".CHR'"CO2 H or tetrazolyl, R1 and R2 are each hydroxyl, halo, C1-4 alkyl, C1-4 alkoxy, acyloxy, --O-glucoside, optionally substituted phenyl or optionally substituted phenyl C1-4 alkoxy; and or a pharmaceutically acceptable salt or ester thereof.
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- Thiol-reactive Fluorescent probes for Protein Labelling
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Cyclisation of N-alkylmaleic acids mediated by acetic anhydride in dimethylacetamide in the presence of traces of cobalt naphthenate has been used for efficient assembly of a range of fluorescent maleimide reagents.The fluorescence responses of these reagents to addition of thiol across the maleimide double bond, and to hydrolysis of the meleimide ring, are described.
- Corrie, John E. T.
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p. 2975 - 2982
(2007/10/02)
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- Heterosubstituted Anthracene-9,10-dione Analogues. The Synthesis and Antitumor Evaluation of 5,8-Bisnaphthothiophene-4,9-diones
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A number of 5,8-bisnaphthothiophene-4,9-diones have been synthesized and evaluated for antitumor activity against L1210 leukemia both in vitro and in vivo.Two of the congeners exhibited in vivo activities quite comparable to that
- Krapcho, Paul A.,Petry, Mary E.,Hacker, Miles P.
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p. 2651 - 2655
(2007/10/02)
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- Aromatic prostaglandin derivatives
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Aromatic prostaglandin derivatives are prepared. These compounds have valuable antiprostaglandin activity specifically inhibiting prostaglandin synthesis and antagonizing diarrhea induced by prostaglandin E2 (PGE2).
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