نتایج جستجو برای: hantzsch synthesis
تعداد نتایج: 409399 فیلتر نتایج به سال:
The four-component Hantzsch reaction provides access to pharmaceutically important dihydropyridines. To expand the utility of this method, we have developed a route under organocatalytic conditions with good yields and excellent ee's. Through catalyst screening, we found that a BINOL-phosphoric acid allowed enantioselective synthesis of six-membered heterocycles with a variety of substitution p...
A straightforward enantiomerically pure synthesis of the heterocyclic core of the D-series GE2270 is reported. The synthetic strategy combines the Hantzsch thiazole's building condensation with a cross-coupling reaction including direct C-H hetarylation to build and connect step-by-step thiazolyl moieties to the 5-bromopicolinate as readily available starting material.
Thiophene containing thiazolyl carbohydrazide on reaction with various aryl isothiocynates yields thiosemicarbazides which were transformed into 1,2,4- substituted thiazoles by Hantzsch synthesis and characterized spectral methods. Most of the synthesized new are found to be promisingly effective against tested bacterial strains exhibited moderate activitytested fungal strains. 1, 2,4- weakly a...
A reinvestigation of a chiral phosphoric-acid-catalyzed four-component Hantzsch enantioselective synthesis polyhydroquinolines reported in 2009 is presented. In our hands, when the reaction was performed with fidelity to original report using enantiopure phosphoric acid catalyst, no enantioselectivity observed. Unlike report, results are backed by baseline separation enantiomers HPLC analyses o...
Abstract: Thiazole or 1,3-thiazole is a distinct heterocyclic compound which incorporates sulphur and nitrogen atoms. It vital framework present in numerous pharmacologically active compounds, be it of natural origin synthetic nature. Many thiazoles having antitumor antiviral activities, originate from microbes marine organisms. A variety drugs, thiazole group, like antimicrobial sulfathiazole,...
Hantzsch esters (1,4-dihydropyridine dicarboxylates) have become, in this century, very versatile reagents for enantioselective organic transformations. They can act as hydride transfer agents to reduce, regioselectively, a variety of multiple bonds, e.g., C=C and C=N, under mild reaction conditions. are excellent the dearomatization heteroaromatic substances, participate readily cascade proces...
a simple and mild one-pot three-component reaction for the preparation 1,4-dihydropyridines has been developed from various aldehyde substrates, 1,3-dicarbonyl compounds (dimedone) and ammonium acetate (hantzsch method) in the presence of a catalytic amount of phospho sulfonic acid (psa) as an efficient and heterogeneous solid acid in etoh at room temperature. preparation of psa is straightforw...
A general process for the high-yielding synthesis of substituted chiral and achiral α-substituted acrylates was achieved through the sequential one-pot combination of a metal-free reductive coupling reaction followed by an Eschenmoser methylenation. The proline catalyzed reaction of Meldrum's acid, aldehydes and Hantzsch ester followed by methylenation was successful with Eschenmoser's salt in ...
An efficient enantioselective synthesis of the chiral polycyclic cholesteryl ester transfer protein (CETP) inhibitor 1 has been developed. The synthesis was rendered practical for large scale via the development of a modified Hantzsch-type reaction to prepare the sterically hindered pyridine ring, enantioselective hydrogenation of hindered ketone 6 utilizing novel BIBOP-amino-pyridine derived R...
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