The impact of microwave-assisted organic synthesis in drug discovery

被引:83
作者
Mavandadi, F
Pilotti, Å
机构
[1] Biotage LLC, Charlottesville, VA 22911 USA
[2] Biotage AB, SE-75318 Uppsala, Sweden
关键词
D O I
10.1016/S1359-6446(05)03695-0
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Microwave-assisted organic synthesis has revolutionized organic synthesis. Small molecules can be built in a fraction of the time required by classical thermal methods. As a result, this technique has rapidly gained acceptance as a valuable tool for accelerating drug discovery and development processes. This article outlines the basic principles behind microwave technology and summarizes recent trends and areas in drug discovery where this technology has made an impact.
引用
收藏
页码:165 / 174
页数:10
相关论文
共 72 条
[1]   Reproducibility across microwave instruments:: Preparation of a set of 24 compounds on a multiwell plate under temperature-controlled conditions [J].
Alcázer, J .
JOURNAL OF COMBINATORIAL CHEMISTRY, 2005, 7 (03) :353-355
[2]   Dioxygen-promoted regioselective oxidative Heck arylations of electron-rich olefins with arylboronic acids [J].
Andappan, MMS ;
Nilsson, P ;
von Schenck, H ;
Larhed, M .
JOURNAL OF ORGANIC CHEMISTRY, 2004, 69 (16) :5212-5218
[3]   A microwave-assisted click chemistry synthesis of 1,4-disubstituted 1,2,3-triazoles via a copper(I)-catalyzed three-component reaction [J].
Appukkuttan, P ;
Dehaen, W ;
Fokin, VV ;
Van der Eycken, E .
ORGANIC LETTERS, 2004, 6 (23) :4223-4225
[4]   Suzuki coupling of aryl chlorides with phenylboronic acid in water, using microwave heating with simultaneous cooling [J].
Arvela, RK ;
Leadbeater, NE .
ORGANIC LETTERS, 2005, 7 (11) :2101-2104
[5]   Cyclic sulfamide HIV-1 protease inhibitors, with sidechains spanning from P2/P2′ to P1/P1′ [J].
Ax, A ;
Schaal, W ;
Vrang, L ;
Samuelsson, B ;
Hallberg, A ;
Karlén, A .
BIOORGANIC & MEDICINAL CHEMISTRY, 2005, 13 (03) :755-764
[6]   Bispyridylamides - coordination chemistry and applications in catalytic reactions [J].
Belda, O ;
Moberg, C .
COORDINATION CHEMISTRY REVIEWS, 2005, 249 (5-6) :727-740
[7]   Catalytic multicomponent synthesis of highly substituted pyrroles utilizing a one-pot Sila-Stetter/Paal-Knorr strategy [J].
Bharadwaj, AR ;
Scheidt, KA .
ORGANIC LETTERS, 2004, 6 (14) :2465-2468
[8]   A microreactor for microwave-assisted capillary (continuous flow) organic synthesis [J].
Comer, E ;
Organ, MG .
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 2005, 127 (22) :8160-8167
[9]   Microwave assisted combinatorial chemistry synthesis of substituted pyridines [J].
Cotterill, IC ;
Usyatinsky, AY ;
Arnold, JM ;
Clark, DS ;
Dordick, JS ;
Michels, PC ;
Khmelnitsky, YL .
TETRAHEDRON LETTERS, 1998, 39 (10) :1117-1120
[10]   A straightforward, one-pot protocol for the preparation of libraries of 2-oxazolines [J].
Crosignani, S ;
Swinnen, D .
JOURNAL OF COMBINATORIAL CHEMISTRY, 2005, 7 (05) :688-696