Parallel Solution-Phase Synthesis of a 2-Aminothiazole Library Including Fully Automated Work-Up

被引：5

作者：

Buchstaller, Hans-Peter ^{[1
]}

Anlauf, Uwe ^{[1
]}

机构：

[1] Merck KGaA, Merck Serono, MS RTC MedChem DA35, MS DTC MD1B Med Chem Darmstadt 1B1, D-64293 Darmstadt, Germany

来源：

COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING | 2011年 / 14卷 / 02期

关键词：

Aminothiazole; combinatorial chemistry; solution phase synthesis; automation; INHIBITORS; DISCOVERY; PROGRESS; DISEASE;

D O I：

10.2174/138620711794474024

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

A straightforward and effective procedure for the solution phase preparation of a 2-aminothiazole combinatorial library is described. Reaction, work-up and isolation of the title compounds as free bases was accomplished in a fully automated fashion using the Chemspeed ASW 2000 automated synthesizer. The compounds were obtained in good yields and excellent purities without any further purification procedure.

引用

页码：104 / 108

页数：5

共 50 条

[31] Solution-phase reductive cyclization of 2-quinoxalinol analogs: Systematic study of parallel synthesis
Wu, Xiang-Hong
Liu, Gang
Zhang, Jing
Wang, Zhan-Guo
Xu, Song
Zhang, Suo-De
Zhang, Liang
Wang, Lin
MOLECULAR DIVERSITY, 2004, 8 (02) : 165 - 174
[32] Application of solution-phase parallel synthesis to preparation of trisubstituted 1,2,4-triazoles
Martin, SW
Romine, JL
Chen, L
Mattson, G
Antal-Zimanyi, IA
Poindexter, GS
JOURNAL OF COMBINATORIAL CHEMISTRY, 2004, 6 (01): : 35 - 37
[33] Solution-phase reductive cyclization of 2-quinoxalinol analogs: Systematic study of parallel synthesis
Xiang-Hong Wu
Gang Liu
Jing Zhang
Zhan-Guo Wang
Song Xu
Suo-De Zhang
Liang Zhang
Lin Wang
Molecular Diversity, 2004, 8 : 165 - 174
[34] Achieving functional group diversity in parallel synthesis: solution-phase synthesis of a library of ureas, carbamates, thiocarbamates, and amides using carbamoylimidazolium salts
Grzyb, Justyna A.
Batey, Robert A.
TETRAHEDRON LETTERS, 2008, 49 (36) : 5279 - 5282
[35] Solution-phase parallel synthesis of a benzoxazinone library using complementary molecular reactivity and molecular recognition (CMR/R) purification technology
Parlow, JJ
Flynn, DL
TETRAHEDRON, 1998, 54 (16) : 4013 - 4031
[36] Parallel synthesis of a library of acylsemicarbazides using a solution-phase one-pot method and their evaluation as crop-protection agents
Grzyb, JA
Dekeyser, MA
Batey, RA
SYNTHESIS-STUTTGART, 2005, (14): : 2384 - 2392
[37] Solution-phase parallel synthesis of 3,5,6-substituted indolin-2-ones
Yang, Tian-Ming
Liu, Gang
JOURNAL OF COMBINATORIAL CHEMISTRY, 2007, 9 (01): : 86 - 95
[38] Microwave-assisted solution-phase parallel synthesis of 2,4,6-trisubstituted pyrimidines
Nie, Aihua
Wang, Jun
Huang, Ziwei
JOURNAL OF COMBINATORIAL CHEMISTRY, 2006, 8 (05): : 646 - 648
[39] An effective methodology for the solution-phase synthesis of fatty acid derivatives of aminosugar library: Development of coupling-purification conditions for parallel reactions
Ravi, Mallikarjun Reddy
Liu, Meizheng
Wang, Wuyi
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2005, 230 : U3385 - U3386
[40] Solution-phase parallel synthesis of a pyridinium pyrazol-3-olate inner salt library using a three-component reaction
Varga, L
Nagy, T
Dormán, G
Kálmán, F
Ürge, L
Darvas, F
JOURNAL OF COMBINATORIAL CHEMISTRY, 2006, 8 (03): : 338 - 343

← 1 2 3 4 5 →