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Synthesis of amino-benzothiaoxazepine-1,1-dioxides utilizing a microwave-assisted, S(N)Ar protocol.


ABSTRACT: The development of a microwave-assisted, intermolecular S(N)Ar protocol for the synthesis of a 126-member benzothiaoxazepine-1,1-dioxide library is reported. Diversification of 12 benzothiaoxazepine-1,1-dioxides was achieved in rapid fashion utilizing a variety of 2° amines and amino alcohols to generate an 80-member library. A second 48-member library was subsequently generated via a two-step alkylation, intermolecular S(N)Ar diversification protocol.

SUBMITTER: Rolfe A 

PROVIDER: S-EPMC3271943 | biostudies-literature | 2011 Nov

REPOSITORIES: biostudies-literature

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Synthesis of amino-benzothiaoxazepine-1,1-dioxides utilizing a microwave-assisted, S(N)Ar protocol.

Rolfe Alan A   Ullah Farman F   Samarakoon Thiwanka B TB   Kurtz Ryan D RD   Porubsky Patrick P   Neuenswander Benjamin B   Lushington Gerald H GH   Santini Conrad C   Organ Michael G MG   Hanson Paul R PR  

ACS combinatorial science 20110908 6


The development of a microwave-assisted, intermolecular S(N)Ar protocol for the synthesis of a 126-member benzothiaoxazepine-1,1-dioxide library is reported. Diversification of 12 benzothiaoxazepine-1,1-dioxides was achieved in rapid fashion utilizing a variety of 2° amines and amino alcohols to generate an 80-member library. A second 48-member library was subsequently generated via a two-step alkylation, intermolecular S(N)Ar diversification protocol. ...[more]

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