Zobrazeno 1 - 10
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pro vyhledávání: '"Nicholas M Leonard"'
Autor:
Nicholas M. Leonard, Jarmila Brunckova
Publikováno v:
Organic Preparations and Procedures International. 44:180-183
Succinimidyl-4-(N-maleimidomethyl)cyclohexane-1-carboxylate (2, SMCC) has found utility in numerous areas of chemistry and biotechnology. The well-established chemoselective reactivity of SMCC has ...
Autor:
Nicholas M. Leonard, Jarmila Brunckova
Publikováno v:
The Journal of Organic Chemistry. 76:9169-9174
A method for the in situ formation of N-trifluoroacetoxy succinimide (TFA-NHS) and its application in the formation of succinimidyl esters is presented. The developed method provides N-trifluoroacetyl and N-maleoyl amino acid succinimidyl esters from
Autor:
Nicholas M. Leonard, K. A. Woerpel
Publikováno v:
The Journal of Organic Chemistry. 74:6915-6923
Nitrogen heterocycles can be prepared by performing ring-expansion reactions of gamma-silyloxy-gamma-lactams, which are available by the annulation reactions of allylic silanes. Nucleophilic substitution of the annulation products and subsequent tran
Autor:
Hing L. Sham, Lisa A. Hasvold, Jerry Cohen, Weibo Wang, Yunsong Tong, Wen-Zhen Gu, Qun Li, Joy Bauch, Saul H. Rosenberg, Tongmei Li, Nicholas M Leonard, Le Wang, Vincent S. Stoll, Haiying Zhang, Nan-Horng Lin, Kennan C. Marsh
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:1571-1574
A pyridyl moiety was introduced into a previously developed series of farnesyltransferase inhibitors containing imidazole and cyanophenyl (such as 4), resulting in potent inhibitors with improved pharmacokinetics.
Publikováno v:
Tetrahedron Letters. 42:8129-8132
Aryl-substituted epoxides undergo smooth rearrangement in the presence of 0.01–0.1 mol% Bi(OTf) 3 · x H 2 O. The rearrangement is regioselective with aryl-substituted epoxides, and products arise from cleavage of the benzylic CO bond. The highl
Autor:
Nicholas M. Leonard, Jarmila Brunckova
Publikováno v:
ChemInform. 43
An improved one-pot synthesis of SMCC (IV), a valuable heterobifunctional linker in pharmaceutical chemistry, is described.
Publikováno v:
Organic Letters. 5:55-57
The chemoselective allylation of acetals using allyltrimethylsilane in ionic liquids is catalyzed by TMS triflate (5.0-20.0 mol %). The reaction proceeds smoothly at room temperature to afford the corresponding homoallyl ether in good yield. Since th
Publikováno v:
ChemInform. 33
Aryl-substituted epoxides undergo smooth rearrangement in the presence of 0.01–0.1 mol% Bi(OTf) 3 · x H 2 O. The rearrangement is regioselective with aryl-substituted epoxides, and products arise from cleavage of the benzylic CO bond. The highl
Autor:
K. A. Woerpel, Nicholas M. Leonard
Publikováno v:
ChemInform. 41
Nitrogen heterocycles can be prepared by performing ring-expansion reactions of γ-silyloxy-γ-lactams, which are available by the annulation reactions of allylic silanes. Nucleophilic substitution of the annulation products and subsequent translacta
Autor:
Charles W. Hutchins, Jerry Cohen, Kennan C. Marsh, David C. Park, Wang Xilu, Gerry Sullivan, Gary T. Wang, Le Wang, Nan-Horng Lin, Vincent S. Stoll, Qun Li, Nicholas M Leonard, Wen-Zhen Gu, Joy Bauch, Haiying Zhang, Saul H. Rosenberg, Hing L. Sham, Yunsong Tong, Clarissa G. Jakob
Publikováno v:
Journal of medicinal chemistry. 47(3)
A novel series of 4-[(4-cyano-2-arylbenzyloxy)-(3-methyl-3H-imidazol-4-yl)methyl]benzonitriles have been synthesized as selective farnesyltransferase inhibitors using structure-based design. X-ray cocrystal structures of compound 20-FTase-HFP and A31