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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]

PMID: 21902243

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