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Solid-phase Synthesis of 2-Substituted-3-(substituted Sulfanyl)-1,2,4-benzothiadiazine 1,1-Dioxide Library by Shingo Makino; Tatsuya Okuzumi; Eiji Nakanishi; Takashi Tsuji is a Chemistry article available to read on EtoBox.

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The first solid-phase synthesis of 2-substituted-3-(substituted sulfanyl)-1,2,4-benzothiadiazine 1,1-dioxides has been developed. Synthesis of the title compounds was achieved as follows: (1) sulfonylation of solid-supported primary amines with 2-nitrobenzenesulfonylchlorides, (2) reduction of the nitro group, (3) cyclization with thiocarbonyldiimidazole (formation of thiourea), (4) S-alkylation or S-arylation of the thiourea. In addition to the excellent purity of the product, a large-size library can be synthesized with the method as this synthesis includes three diversity points.

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Author

Shingo Makino; Tatsuya Okuzumi; Eiji Nakanishi; Takashi Tsuji

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0040-4039)

Published

2002

Language

EN

Field

Chemistry (Physical Sciences)