ACS Combinatorial Science
Page 18 of 19
1
2
3
4
5
6
7
8
9
(11) Lin, Q.; Meloni, D.; Pan, Y.; Xia, M.; Rodgers, J.; Shepard, S.; Li, M.; Galya, L.; Metcalf,
B.; Yue, T.ꢀY.; Liu, P.; Zhou, J. Enantioselective Synthesis of Janus Kinase Inhibitor
INCB018424 via an Organocatalytic AzaꢀMichael Reaction. Org Lett 2009, 11, 1999–
2002.
(12) Huisgen, R. Centenary Lecture: 1,3ꢀDipolar Cycloadditions. Proc. Chem. Soc. 1961, 357–
396.
10
11
12
13
14
15
16
17
18
19
20
21
22
23
24
25
26
27
28
29
30
31
32
33
34
35
36
37
38
39
40
41
42
43
44
45
46
47
48
49
50
51
52
53
54
55
56
57
58
59
60
(13) Tornøe, C. W.; Christensen, C.; Meldal, M. Peptidotriazoles on Solid Phase:ꢀ [1,2,3]ꢀ
Triazoles by Regiospecific Copper(I)ꢀCatalyzed 1,3ꢀDipolar Cycloadditions of Terminal
Alkynes to Azides. J. Org. Chem. 2002, 67, 3057–3064.
(14) Rostovtsev, V. V.; Green, L. G.; Fokin, V. V.; Sharpless, K. B. A Stepwise Huisgen
Cycloaddition Process: Copper(I)ꢀCatalyzed Regioselective “Ligation” of Azides and
Terminal Alkynes. Angew. Chem. Int. Ed. 2002, 41, 2596–2599.
(15) Kolb, H. C.; Finn, M. G.; Sharpless, K. B. Click Chemistry: Diverse Chemical Function
from a Few Good Reactions. Angew. Chem. Int. Ed. 2001, 40, 2004–2021.
(16) Bräse, S.; Gil, C.; Knepper, K.; Zimmermann, V. Organische Azide – explodierende
Vielfalt bei einer einzigartigen Substanzklasse. Angew. Chem. 2005, 117, 5320–5374.
(17) Sonogashira, K. Development of Pd–Cu Catalyzed CrossꢀCoupling of Terminal
Acetylenes with sp2ꢀCarbon Halides. J. Organomet. Chem. 2002, 653, 46–49.
(18) Gehringer, M.; Pfaffenrot, E.; Bauer, S.; Laufer, S. A. Design and Synthesis of Tricyclic
JAK3 Inhibitors with Picomolar Affinities as Novel Molecular Probes. ChemMedChem
2014, 9, 277–281.
(19) Thibault, C.; L’Heureux, A.; Bhide, R. S.; Ruel, R. Concise and Efficient Synthesis of 4ꢀ
Fluoroꢀ1Hꢀpyrrolo[2,3ꢀB]pyridine. Org. Lett. 2003, 5, 5023–5025.
(20) Alvarez, S. G.; Alvarez, M. T. A Practical Procedure for the Synthesis of Alkyl Azides at
Ambient Temperature in Dimethyl Sulfoxide in High Purity and Yield. Synthesis 1997,
1997, 413–414.
(21) GoddardꢀBorger, E. D.; Stick, R. V. An Efficient, Inexpensive, and ShelfꢀStable
Diazotransfer Reagent:ꢀ Imidazoleꢀ1ꢀSulfonyl Azide Hydrochloride. Org. Lett. 2007, 9,
3797–3800.
(22) Fischer, N.; GoddardꢀBorger, E. D.; Greiner, R.; Klapötke, T. M.; Skelton, B. W.;
Stierstorfer, J. Sensitivities of Some Imidazoleꢀ1ꢀSulfonyl Azide Salts. J. Org. Chem.
2012, 77, 1760–1764.
(23) Merkul, E.; Klukas, F.; Dorsch, D.; Grädler, U.; Greiner, H. E.; Müller, T. J. J. Rapid
Preparation of Triazolyl Substituted NHꢀHeterocyclic Kinase Inhibitors via OneꢀPot
Sonogashira coupling–TMSꢀdeprotection–CuAAC Sequence. Org. Biomol. Chem. 2011,
9, 5129–5136.
(24) Bauer, S. M.; Gehringer, M.; Laufer, S. A. A Direct EnzymeꢀLinked Immunosorbent
Assay (ELISA) for the Quantitative Evaluation of Janus Kinase 3 (JAK3) Inhibitors. Anal.
Methods 2014, 6, 8817–8822.
(25) Zhu, K.; Borrelli, K. W.; Greenwood, J. R.; Day, T.; Abel, R.; Farid, R. S.; Harder, E.
Docking Covalent Inhibitors: A Parameter Free Approach To Pose Prediction and Scoring.
J. Chem. Inf. Model. 2014, 54, 1932–1940.
(26) Manetsch, R.; Krasiński, A.; Radić, Z.; Raushel, J.; Taylor, P.; Sharpless, K. B.; Kolb, H.
C. In Situ Click Chemistry:ꢀ Enzyme Inhibitors Made to Their Own Specifications. J. Am.
Chem. Soc. 2004, 126, 12809–12818.
ACS Paragon Plus Environment
17