PdII-Catalyzed methoxylation of C(sp3)-H bonds adjacent to benzoxazoles and benzothiazoles
The Pd(OAc)2/PhI(OAc)2 catalyst system promotes the highly regioselective dehydrogenative methoxylation of a C(sp3)-H bond adjacent to benzoxazole and benzothiazole rings. The title transformation constitutes the first example of a Pd-catalyzed C(sp3)-H activating methoxylation at the proximal-selective α-position with regard to a directing auxiliary and provides expedient access to an important class of azole-decorated methyl ethers (up to 90% isolated yield). The synthetic practicality of the methodology was demonstrated by achieving α-methoxyacetic acids via the elimination of the benzoxazole auxiliaries and by obtaining the precursor of an O-methylated Breslow intermediate.
Kumar, Jogendra,Gupta, Aniket,Bhadra, Sukalyan
supporting information
p. 3314 - 3318
(2019/04/01)
Palladium(II)/N-heterocyclic carbene-catalyzed direct C-H acylation of heteroarenes with N-acylsaccharins
N-Acylsaccharin represents a facile acyl group transfer agent to heteroarenes in the presence of Pd(II)/NHC complexes appended with a pyrene unit. Catalytic acylation of heteroarenes was enhanced by the noncovalent interaction between the pyrene unit and
Karthik, Shanmugam,Gandhi, Thirumanavelan
p. 5486 - 5489
(2017/11/06)
Synthesis of 2-Keto(hetero)aryl Benzox(thio)azoles through Base Promoted Cyclization of 2-Amino(thio)phenols with α,α-Dihaloketones
An interesting base-promoted protocol for the synthesis of 2-keto(hetero)aryl benzox(thi)azoles has been developed. Starting from commercially available 2-amino(thio)phenols and α,α-dihaloketones, moderate to good yields of the corresponding heterocycles can be achieved. Notably, only EtNH2 was required as the promoter here, and the reaction can be easily performed on a large scale.
A one-pot hypoiodite catalysed oxidative cycloetherification approach to benzoxazoles
A practical one-pot hypoiodite catalysed oxidative cyclization approach to synthesize α-ketobenzoxazole derivatives was successfully developed. This operationally simple protocol utilizes easily-accessible starting materials and has a broad substrate scope with excellent yields. This journal is the Partner Organisations 2014.
Ruthenium catalyzed hydrohydroxyalkylation of isoprene with heteroaromatic secondary alcohols: Isolation and reversible formation of the putative metallacycle intermediate
Heteroaromatic secondary alcohols react with isoprene to form products of hydrohydroxyalkylation in the presence of ruthenium(0) catalysts generated from Ru3(CO)12 and tricyclohexylphosphine, enabling direct conversion of secondary to tertiary alcohols in the absence of premetalated reagents or stoichiometric byproducts. The putative oxaruthenacycle intermediate has been isolated and characterized, and reversible metallacycle formation has been demonstrated.
Park, Boyoung Y.,Montgomery, T. Patrick,Garza, Victoria J.,Krische, Michael J.
supporting information
p. 16320 - 16323
(2013/12/04)
PIPERAZINYL DERIVATIVES USEFUL AS MODULATORS OF THE NEUROPEPTIDE Y2 RECEPTOR
The present invention is directed to piperidinyl and piperazinyl derivatives of formula (II) useful as inhibitors of the NPY Y2 receptor, pharmaceutical compositions comprising said compounds, processes for the preparation of said compounds and the use of said compounds for the treatment and / or prevention of disorders, diseases and conditions mediated by the NPY Y2 receptor.
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Page/Page column 72
(2009/07/18)
Antiviral agents. 1. Benzothiazole and benzoxazole analogs of 2-(alpha-hydroxybenzyl)benzimidazole.
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Gualtiere,Brody,Fieldsteel,Skinner
p. 546 - 549
(2007/10/08)
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