Zobrazeno 1 - 10
of 38
pro vyhledávání: '"Francis A. J. Kerdesky"'
Autor:
Bhadra H. Shelat, Eric A. Voight, Steven M. Hannick, Jerome F. Daanen, Kort Michael E, Francis A. J. Kerdesky, Daniel J. Plata
Publikováno v:
Tetrahedron Letters. 51:5904-5907
Starting from a variety of substituted chroman-4-ones, a highly enantioselective CBS reduction using in situ-generated B–H catalyst gave ( S )-chroman-4-ols. Azide inversion and reduction gave crude ( R )-chroman-4-amines, which could be purified w
Autor:
David M. Barnes, Jufang Barkalow, Yong Chen, Francis A. J. Kerdesky, John E. Hengeveld, Anthony R. Haight, Bryan Macri, Ashok K. Gupta, Agnes Pal, Brian J. Kotecki
Publikováno v:
Organic Process Research & Development. 13:225-229
The impact of entropic effects on the classical salt resolution of a 2-arylpyrrolidine is described. We have found that the crystallization of a racemic mixture of the base with tartaric acid led to a salt in which the undesired enantiomer is incorpo
Autor:
John C. Tolle, Francis A. J. Kerdesky, Seble Wagaw, Calvin L. Becker, Weifeng Wang, Kenneth M. Engstrom
Publikováno v:
Organic Process Research & Development. 12:1114-1118
A convergent, scalable process was developed for the synthesis of adamantane 11-β-hydroxysteroid dehydrogenase-1 inhibitors E-4-(2-methyl-2-(4-(5-(trifluoromethyl)pyridin-2-yl)piperazin-1-yl)propionylamino)adamantane-1-carboxylic acid (1) and E-4-(2
Autor:
John E. Lallaman, Jianguo Ji, Wenke Li, Howard E. Morton, Ji Zhang, Francis A. J. Kerdesky, M. Robert Leanna
Publikováno v:
Organic Process Research & Development. 10:512-517
An efficient chemical process for the multikilogram synthesis of ABT-963 (3) is described. The potent and selective COX-2 inhibitor was prepared in four steps in 36% overall isolated yield from commercially available 3,4-difluoroaniline (4). The chem
Autor:
M. Robert Leanna, Eric J. Stoner, Maureen A. McLaughlin, Steven L. Condon, Steven A. King, Francis A. J. Kerdesky, Steven J. Wittenberger, Matthew J. Peterson, Michael Rasmussen, Daniel J. Plata
Publikováno v:
Tetrahedron. 60:10171-10180
A practical and efficient synthesis of ketolide antibiotic cethromycin (ABT-773) (1) is described. An effective protection strategy allows high yielding, regioselective C6-O-alkylation and subsequent stereoselective modification of the erythromycin n
Autor:
Gregory S. Wayne, John E. Lallaman, Lakshmi Bhagavatula, Jonathan P. Pease, Ramiya H. Premchandran, Steven A. King, William H. Arnold, Francis A. J. Kerdesky, Howard E. Morton, Sou-Jen Chang
Publikováno v:
Organic Process Research & Development. 6:869-875
An efficient and practical synthesis of 2‘-O-benzoyl-3-keto-6-O-propargyl-11,12-carbamoyl erythromycin A (4) is described. The semisynthetic macrolide was prepared on large scale in seven steps in 38% overall isolated yield from the readily availab
Autor:
Michael Fitzgerald, Michael S. Allen, Francis A. J. Kerdesky, Lakshmi Bhagavatula, J. A. Menzia, Timothy L. Stuk, Anthony R. Haight, Timothy A. Robbins, Shyamal I. Parekh, Steven M. Hannick, and David Scarpetti, Jien-Heh J. Tien
Publikováno v:
Organic Process Research & Development. 3:94-100
The reduction of (5S)-2-amino-5-dibenzylamino-4-oxo-1,6-diphenylhex-2-ene was optimized for diastereoselectivity and overall conversion to (2S,3S,5S)-5-amino-2-dibenzylamino-3-hydroxy-1,6-diphenylhexane (2a). A two-step reduction sequence is describe
Publikováno v:
Synthetic Communications. 26:1007-1013
A novel and efficient synthesis of A-81988, an angiotensin II receptor antagonist, is described. The key step utilizes a palladium-catalyzed biaryl coupling between a phenylboronic acid derivative and N-trityl-5-(2-bromophenyl)tetrazole.
Autor:
Francis A. J. Kerdesky, Louis S. Seif
Publikováno v:
Synthetic Communications. 25:4081-4086
The hydrogenation of halothiazoles is described. The best results were obtained utilizing 10% palladium on carbon as catalyst at four atmospheres of pressure with the bromide derivatives.
Autor:
Francis A. J. Kerdesky, Louis S. Seif
Publikováno v:
Synthetic Communications. 25:2639-2645
A novel and efficient synthesis of 5-(hydroxymethyl) thiazole, an important synthon for the preparation of biologically active compounds, is described. The research also provides additional insight into the properties of halothiazoles.