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S(N)Ar-based, facile synthesis of a library of benzothiaoxazepine-1,1'-dioxides.

ABSTRACT: The construction of a library of benzothiaoxazepine-1,1'-dioxides utilizing a one-pot, S(N)Ar diversification-ODCT(50) scavenging protocol is reported. This protocol combines microwave irradiation to facilitate the reaction, in conjunction with a soluble ROMP-derived scavenger (ODCT) to afford the desired products in good overall purity. Utilizing this protocol, a 78-member library was successfully synthesized and submitted for biological evaluation.

SUBMITTER: Rolfe A 

PROVIDER: S-EPMC3098767 | biostudies-literature | 2010 Nov

REPOSITORIES: biostudies-literature

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S(N)Ar-based, facile synthesis of a library of benzothiaoxazepine-1,1'-dioxides.

Rolfe Alan A   Samarakoon Thiwanka B TB   Klimberg Sarra V SV   Brzozowski Marek M   Neuenswander Benjamin B   Lushington Gerald H GH   Hanson Paul R PR  

Journal of combinatorial chemistry 20100929 6

The construction of a library of benzothiaoxazepine-1,1'-dioxides utilizing a one-pot, S(N)Ar diversification-ODCT(50) scavenging protocol is reported. This protocol combines microwave irradiation to facilitate the reaction, in conjunction with a soluble ROMP-derived scavenger (ODCT) to afford the desired products in good overall purity. Utilizing this protocol, a 78-member library was successfully synthesized and submitted for biological evaluation. ...[more]

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