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Träfflista för sökning "WFRF:(Wakchaure Prasad B.) "

Sökning: WFRF:(Wakchaure Prasad B.)

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1.
  • Nandi, Ganesh C., et al. (författare)
  • Pd-catalyzed C-N coupling of vinylbromides and sulfonimidamides : a facile synthesis of N '-vinylsulfonimidamides
  • 2015
  • Ingår i: RSC Advances. - : Royal Society of Chemistry (RSC). - 2046-2069. ; 5:76, s. 62084-62090
  • Tidskriftsartikel (refereegranskat)abstract
    • N'-Vinyl sulfonimidamides have been synthesized through a Pd-catalyzed C-N cross coupling between the N'-(imine nitrogen) of N'-deprotected sulfonimidamides and vinyl bromides. The hitherto unreported products were obtained in moderate to excellent yield, and the C-C double bond geometry of the vinylic substrates were retained during the course of reaction. Single crystal X-ray crystallographic analysis confirmed the product structure. Furthermore, we demonstrate that the formed N'-vinyl sulfonimidamides could undergo hydrogenation with Pd-C/H-2 to provide N'-alkyl sulfonimidamides.
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2.
  • Wakchaure, Prasad B., et al. (författare)
  • Synthesis of enantiopure angiotensin II type 2 receptor [AT(2)R] antagonist EMA401
  • 2015
  • Ingår i: Tetrahedron. - : Elsevier BV. - 0040-4020 .- 1464-5416. ; 71:38, s. 6881-6887
  • Tidskriftsartikel (refereegranskat)abstract
    • We report a facile synthesis of the angiotensin II type 2 receptor antagonist EMA401, which recently passed phase II clinical trials, in high overall yield. The synthesis of the key phenylalanine intermediate involved the formation of an a-nitro cinnamic ester and its reduction followed by a Pictet-Spengler cyclization, which furnished the tetrahydroisoquinoline core structure. Next, EMA401 was separated from its enantiomer EMA402 by four recrystalizations of a diastereomeric salt in 98% ee. All steps were performed on gram scale with emphasis on avoiding column purification and using readily available low cost starting materials and reagents.
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  • Resultat 1-2 av 2

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