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Novel 2,2-dioxide-4,4-disubstituted-1,3-H-2,1,3-benzothiadiazines as non-nucleoside reverse transcriptase inhibitors

✍ Scribed by Jeffrey W Corbett; Lisa A Gearhart; Soo S Ko; James D Rodgers; Beverly C Cordova; Ronald M Klabe; Susan K Erickson-Viitanen

Book ID
104364954
Publisher
Elsevier Science
Year
2000
Tongue
English
Weight
112 KB
Volume
10
Category
Article
ISSN
0960-894X

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✦ Synopsis

AbstractÐBenzothiadiazine non-nucleoside reverse transcriptase inhibitors (NNRTIs) of HIV have been synthesized via a novel process to aord active inhibitors, with the most potent compound exhibiting an IC 90 =180 nM in a whole cell assay. The 2,2dioxide-1H-2,1,3-benzothiadiazine ring system was constructed in one step from 2-amino-5-chlorobenzonitrile.

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ChemInform Abstract: Novel 2,2-Dioxide-4
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A simple method for the preparation of 4,4-disubstituted-3,4-dihydro-1H-2,1,3-benzothiadiazine 2,2dioxides is described. Treatment of N-sulfonyl ketimines 2 and 3 with different carbon nucleophiles afforded the corresponding of 4,4-disubstituted-3,4-dihydro-1H-2,1,3-benzothiadiazine 2,2-dioxides 1 i

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