A single-reagent-driven multistep one-pot preparation of thiazolines and 1,3-thiazines from aldoximes, nitriles, and carboxylic acids
N-(ω-Bromoalkyl)dichlorothiophosphoramidates have been designed as a new class of reagent for the single-reagent-driven multistep preparation of 2-substituted thiazolines and 1,3-thiazines from ald-oximes, nitriles, or carboxylic acids. A wide range of substrates both aromatic as well as aliphatic were investigated and found suitable for the developed protocol.
Identification of Adenosine Deaminase Inhibitors by Metal-binding Pharmacophore Screening
Adenosine deaminase (ADA) is a human mononuclear Zn2+ metalloenzyme that converts adenosine to inosine. ADA is a validated drug target for cancer, but there has been little recent work on the development of new therapeutics against this enzyme. The lack of new advancements can be partially attributed to an absence of suitable assays for high-throughput screening (HTS) against ADA. To facilitate more rapid drug discovery efforts for this target, an in vitro assay was developed that utilizes the enzymatic conversion of a visibly emitting adenosine analogue to the corresponding fluorescent inosine analogue by ADA, which can be monitored via fluorescence intensity changes. Utilizing this assay, a library of ~350 small molecules containing metal-binding pharmacophores (MBPs) was screened in an HTS format to identify new inhibitor scaffolds against ADA. This approach yielded a new metal-binding scaffold with a Ki value of 26±1 μM.
Adamek, Rebecca N.,Ludford, Paul,Duggan, Stephanie M.,Tor, Yitzhak,Cohen, Seth M.
supporting information
p. 2151 - 2156
(2020/10/19)
Transformation of anionically activated trifluoromethyl groups to heterocycles under mild aqueous conditions
The (hetero)aromatic trifluoromethyl group is present in many biologically active molecules and is generally considered to be chemically stable. In this paper, a convenient one-step synthesis of C-C linked aryl-heterocycles or heteroaryl-heterocycles in good to excellent yields via the reaction of anionically activated trifluoromethyl groups with amino nucleophiles containing a second NH, OH, or SH nucleophile in 1 N sodium hydroxide is reported. The method has high functional group tolerability and is potentially useful in parallel synthesis.
Qiao, Jennifer X.,Wang, Tammy C.,Hu, Carol,Li, Jianqing,Wexler, Ruth R.,Lam, Patrick Y. S.
supporting information; experimental part
p. 1804 - 1807
(2011/06/19)
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