Total Synthesis of (±)-Herbindole B and (±)-cis-Trikentrin B
摘要:
Herbindole B and cis-trikentrin B are naturally occurring indoles having the unusual and synthetically challenging pattern of carbon substitution at the 4-7 and 5-7 positions, respectively, with no substitution at the 1-3 positions. The total syntheses of these polyalkylated indoles have been achieved in 19 and 12 steps, respectively. The synthesis of herbindole B relies on two iterations of a quinine monoimine Diels-Alder reaction, while cis-trikentrin B uses a single cycloaddition of a suitable quinone monolmine. Indolization of the adducts provides suitably substituted benzopyrrole nuclei for elaboration to the natural products.
A Novel Safety-Catch Linker for the Solid-Phase Synthesis of Amides and Esters
摘要:
[GRAPHICS]A new safety catch linker for solid phase organic synthesis is described. Synthesis and attachment of the linker to the solid phase was achieved via a simple and high yielding strategy. The linker was exemplified by acylation to form unactivated amides, activation of the linker, and cleavage to release acyl moieties. Acids, amides, or esters were released under mild conditions and with exceptionally high purity. The reactivities of unactivated and activated amides are compared.
Disclosed herein are bifunctional molecules which inhibit HIV entry into the target cell. Also disclosed are novel anti-HIV therapeutics for treatment of patients infected by HIV, including non-B and multi-drug resistant strains.
US8828931B2
申请人:——
公开号:US8828931B2
公开(公告)日:2014-09-09
[EN] BIFUNCTIONAL MOLECULES FOR INHIBITING HIV ENTRY<br/>[FR] MOLÉCULES BIFONCTIONNELLES DESTINÉES À INHIBER LA PÉNÉTRATION DU VIH
申请人:NEW YORK BLOOD CT INC
公开号:WO2009155064A1
公开(公告)日:2009-12-23
Disclosed herein are bifunctional molecules which inhibit HIV entry into the target cell. Also disclosed are novel anti-HIV therapeutics for treatment of patients infected by HIV, including non-B and multi-drug resistant strains.
A Novel Safety-Catch Linker for the Solid-Phase Synthesis of Amides and Esters
作者:Matthew H. Todd、Steven F. Oliver、Chris Abell
DOI:10.1021/ol990785h
日期:1999.10.1
[GRAPHICS]A new safety catch linker for solid phase organic synthesis is described. Synthesis and attachment of the linker to the solid phase was achieved via a simple and high yielding strategy. The linker was exemplified by acylation to form unactivated amides, activation of the linker, and cleavage to release acyl moieties. Acids, amides, or esters were released under mild conditions and with exceptionally high purity. The reactivities of unactivated and activated amides are compared.