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Solid-phase synthesis of 2-substituted-3-(substituted sulfanyl)-1,2,4-benzothiadiazine 1,1-dioxide library

✍ Scribed by Shingo Makino; Tatsuya Okuzumi; Eiji Nakanishi; Takashi Tsuji

Publisher
Elsevier Science
Year
2002
Tongue
French
Weight
91 KB
Volume
43
Category
Article
ISSN
0040-4039

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✦ Synopsis

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.

📜 SIMILAR VOLUMES

Facile synthesis of 4-substituted 3,4-di
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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