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Facile (triazolyl)methylation of MACOS-derived benzofused sultams utilizing ROMP-derived OTP reagents.


ABSTRACT: A combination of MACOS scale-out and ROMP-derived oligomeric triazole phosphates (OTP(n)) have been successfully utilized for the preparation of a 106-member library of triazole containing benzothiaoxazepine-1,1-dioxides. This report demonstrates the utilization of a suite of soluble OTP(n) reagents for facile (triazolyl)methylation of 10 MACOS-derived sultam scaffolds in purification-free process for parallel synthesis of small molecule collections for HTS.

SUBMITTER: Faisal S 

PROVIDER: S-EPMC3656824 | biostudies-literature | 2012 Apr

REPOSITORIES: biostudies-literature

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Facile (triazolyl)methylation of MACOS-derived benzofused sultams utilizing ROMP-derived OTP reagents.

Faisal Saqib S   Ullah Farman F   Maity Pradip K PK   Rolfe Alan A   Samarakoon Thiwanka B TB   Porubsky Patrick P   Neuenswander Benjamin B   Lushington Gerald H GH   Basha Fatima Z FZ   Organ Michael G MG   Hanson Paul R PR  

ACS combinatorial science 20120305 4


A combination of MACOS scale-out and ROMP-derived oligomeric triazole phosphates (OTP(n)) have been successfully utilized for the preparation of a 106-member library of triazole containing benzothiaoxazepine-1,1-dioxides. This report demonstrates the utilization of a suite of soluble OTP(n) reagents for facile (triazolyl)methylation of 10 MACOS-derived sultam scaffolds in purification-free process for parallel synthesis of small molecule collections for HTS. ...[more]

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