Highly Stereoselective Synthesis of Imidazolidines through the Palladium(0)‐Catalyzed Three‐Component Reaction of 2,3‐Allenylamines, Organic Halides, and Imines
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DOI: 10.1002/cctc.201601345
Abstract: A new and efficient method for the synthesis of polysubstituted imidazolidines through the Pd0‐catalyzed double addition/cyclization of 2,3‐allenylamines with aryl iodides and imines was explored. This catalytic reaction afforded the desired products in good yields… read more here.
Keywords: highly stereoselective; imidazolidines palladium; stereoselective synthesis; synthesis imidazolidines ... See more keywords
Stereoselective synthesis of 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-one derivatives as PIM kinase inhibitors inspired from marine alkaloids.
Sign Up to like & getrecommendations! Published in 2022 at "Chirality"
DOI: 10.1002/chir.23501
Abstract: We previously demonstrated that natural product-inspired 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-ones derivatives delivered potent and selective PIM kinases inhibitors however with non-optimal ADME/PK properties and modest oral bioavailability. Herein, we describe a structure-based scaffold decoration and a stereoselective approach… read more here.
Keywords: synthesis dihydropyrrolo; dihydropyrrolo pyrazin; pyrazin one; synthesis ... See more keywords
Stereoselective Synthesis of Tetrahydroisoquinolines from Chiral 4-Azaocta-1,7-diynes and 4-Azaocta-1,7-enynes
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DOI: 10.1002/ejoc.201901590
Abstract: We thank the continued financial support from the Ministerio de Economia y Competitividad (MINECO; project CTQ2014-53695-P, CTQ2014-51912-REDC, CTQ2016-81797-REDC, CTQ2017-85093-P), Ministerio de Ciencia, Innovacion y Universidades (RED2018-102387-T), FEDER, the Generalitat Valenciana (PROMETEOII/2014/017), ant the University of… read more here.
Keywords: chiral azaocta; diynes azaocta; stereoselective synthesis; synthesis tetrahydroisoquinolines ... See more keywords
Highly Stereoselective Synthesis of New Aziridines via Baldwin Rearrangement and Their Potential Biological Activities
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DOI: 10.1002/jhet.2548
Abstract: An atom-economical conversion of N-substituted isoxazoline derivatives to new N-substituted aziridines has been described using microwave irradiation through Baldwin rearrangement. N-substituted isoxazoline derivatives have been synthesized using a variety of nitrones and alkynes via 1,3-dipolar… read more here.
Keywords: highly stereoselective; synthesis new; stereoselective synthesis; baldwin rearrangement ... See more keywords
Stereoselective Synthesis of Pear Ester
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DOI: 10.1007/s10600-017-2191-0
Abstract: A simple two-step synthesis of ethyl-(2E,4Z)-deca-2,4-dienoate based on Fe-catalyzed cross-coupling of ethyl-(2E,4Z)-5-chloropenta-2,4-dienoate, which was obtained via one-pot oxidation and olefination of readily available (2Z)-3-chloroprop-2-en-1-ol by n-pentylmagnesiumbromide, was developed. read more here.
Keywords: synthesis pear; stereoselective synthesis; chemistry; pear ester ... See more keywords
Regio- and stereoselective synthesis of new spiro-isoxazolidines via 1,3-dipolar cycloaddition
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DOI: 10.1016/j.arabjc.2014.05.028
Abstract: Abstract New spiro-isoquinolinediones were prepared by regio- and stereoselective 1,3-dipolar cycloaddition of ( E )-4-arylidene- N -methyl-isoquinoline-1,3-dione derivatives 1a – d with C -aryl- N -phenylnitrones 2e – g . NMR studies confirmed that only… read more here.
Keywords: stereoselective synthesis; dipolar cycloaddition; new spiro; regio stereoselective ... See more keywords
An Auxiliary Approach for the Stereoselective Synthesis of Topologically Chiral Catenanes
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DOI: 10.1016/j.chempr.2019.03.008
Abstract: Summary Catenanes, molecules in which two rings are threaded through one another like links in a chain, can form as two structures related like an object and its mirror image but otherwise identical if the… read more here.
Keywords: synthesis topologically; topologically chiral; chiral catenanes; stereoselective synthesis ... See more keywords
Asymmetric Radical Cyclopropanation of Dehydroaminocarboxylates: Stereoselective Synthesis of Cyclopropyl α-Amino Acids.
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DOI: 10.1016/j.chempr.2021.03.002
Abstract: A catalytic radical process has been developed for asymmetric cyclopropanation of dehydroaminocarboxylates with in situ-generated α-aryldiazomethanes via Co(II)-based metalloradical catalysis (MRC). Through fine-tuning the environments of D 2-symmetric chiral amidoporphyrin platform as the supporting ligands,… read more here.
Keywords: stereoselective synthesis; amino; cyclopropanation dehydroaminocarboxylates; cyclopropanation ... See more keywords
Stereoselective synthesis of novel 2'-(S)-CCG-IV analogues as potent NMDA receptor agonists.
Sign Up to like & getrecommendations! Published in 2020 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2020.113099
Abstract: We developed a versatile stereoselective route for the synthesis of new 2'-(S)-CCG-IV analogues. The route allows for late stage diversification and thereby provides access to a great variety of conformationally restricted cyclopropyl glutamate analogues. A… read more here.
Keywords: nmda receptor; stereoselective synthesis; receptor agonists; ccg analogues ... See more keywords
A new stereoselective synthesis of biologically active di- and trienoic acids containing a (1Z,5Z)-diene moiety
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DOI: 10.1016/j.mencom.2017.05.005
Abstract: Natural (5Z,9Z)-dienoic acids and key precursors of biologically active trienoic acids were prepared in high yields and with high stereoselectivity using cross-cyclomagnesiation of terminal and oxygenated 1,2-dienes with EtMgBr in the presence of Mg metal… read more here.
Keywords: stereoselective synthesis; active trienoic; new stereoselective; biologically active ... See more keywords
Efficient and stereoselective synthesis of (S)-α-propargylglycine derivatives from allenylboronic acid
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DOI: 10.1016/j.mencom.2019.09.006
Abstract: The Petasis–Mannich reaction of allenylboronic acid with glyoxylic acid and (S)-1-phenylethylamine diastereoselectively leads to N-substituted propargylglycine of high optical purity in good yield. This product can be further subjected to esterification followed by bioconjugate synthesis… read more here.
Keywords: allenylboronic acid; propargylglycine; stereoselective synthesis; synthesis propargylglycine ... See more keywords