Zobrazeno 1 - 10
of 29
pro vyhledávání: '"Michael H. Kress"'
Autor:
Allen C. Templeton, Majid Mahjour, Wei Xu, Dina Zhang, Timothy J. Maguire, Michael H. Kress, Filippos Kesisoglou, Lawrence A. Rosen, Maria T. Cruanes
Publikováno v:
Journal of Pharmaceutical Sciences. 103:1811-1818
Telcagepant potassium salt(MK-0974) is an oral calcitonin gene-related peptide receptor inhibitor investigated for the treatment of acute migraine. Under gastric pH conditions, the salt rapidly gels, then converts to an insoluble neutral form that cr
Autor:
Andrew W. Gibson, Fouzia Machrouhi, Doug E. Frantz, Michael H. Kress, Cameron J. Cowden, Norihiro Ikemoto, Todd D. Nelson, Anthony Alorati, Brian C. Bishop, Karsten Menzel, Matthew S. Bodenstein
Publikováno v:
Organic Process Research & Development. 13:519-524
As part of Merck’s continued research effort on inflammation and pain, a safe synthesis of an orally bioavailable and CNS penetrant bradykinin 1 antagonist was developed and demonstrated on kilogram scale. The key step included a novel regioselecti
Publikováno v:
Tetrahedron Letters. 49:415-418
Regioselective halogen/metal exchange reactions using isopropylmagnesium chloride were studied on 3-substituted 1,2,5-tribromoarenes. Seven examples are given.
Autor:
Paul M. Mills, Lisa DiMichele, Karsten Menzel, Doug E. Frantz, Michael H. Kress, Todd D. Nelson
Publikováno v:
Synlett. 2006:1948-1952
Regioselective halogen-metal exchange reactions using isopropylmagnesium chloride were carried out on 3-substituted 1,2-dibromo arenes. Eleven examples are given.
Autor:
Todd D. Nelson, Michael H. Kress, Karsten Menzel, Ethan L. Fisher, Doug E. Frantz, Lisa DiMichele
Publikováno v:
The Journal of Organic Chemistry. 71:2188-2191
A facile protocol for the synthesis of 1,2-dibromoarenes is described. A standard ortho-lithiation/bromination procedure, when applied to bromoarenes, resulted in poor yields of the corresponding 1,2-dibromoarenes (13-62% yield). However, transmetala
Autor:
Aaron Moment, Todd D. Nelson, Osama Sudah, Paul Fernandez, Michael H. Kress, Matthew R. Hickey, Stephen D. Rodgers, Mahmoud S. Kaba, Shawn P. Allwein
Publikováno v:
Organic Process Research & Development. 9:764-767
A scalable process for a pilot plant synthesis of methyl 2-bromo-6-chlorobenzoate (1) is described. The strategy employed for the synthesis hinged on the esterification of the sterically encumbered parent acid produced through an o-lithiation/carboxy
Autor:
John Y. L. Chung, Louis Matty, George Zhou, Fuh-Rong Tsay, Michael H. Kress, Raymond Cvetovich, M. David Weingarten, Joseph S. Amato, Zhen Li
Publikováno v:
The Journal of Organic Chemistry. 70:8560-8563
A practical synthesis of benzisoxazole 1 and its conversion to α-aryloxyisobutyric acid 2 using 1,1,1-trichloro-2-methyl-2-propanol (chloretone) was developed. Benzisoxazole 1 was formed in high yields by the action of either methanesulfonyl chlorid
Publikováno v:
Tetrahedron Letters. 46:1731-1734
A general regioselective synthesis of 2,4-dialkyl resorcinols from ethoxymethylenemalonate ethyl ester and dialkyl ketones is reported.
Publikováno v:
Synlett. :255-258
The synthesis of S-dodecyltrifluorothioacetate and its application to trifluoroacetylation of amino acids under aqueous conditions are described. This reagent afforded good isolated yields (71-92%) of the N-trifluoroacetyl derivatives via an operatio
Autor:
Ulf H. Dolling, Michael H. Kress, Shawn P. Allwein, Todd D. Nelson, Elizabeth A. Secord, Andrew Martins, Jeffrey V. Mitten
Publikováno v:
Synlett. 2004:2489-2492
A convenient route to 1-aminocyclopropane-1-carboxylic acid (1, ACC) and N-protected derivatives was developed. This route utilizes a bisalkylation of an O-benzyl glycine derived imine followed by global deprotection via hydrogenation. Direct isolati