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
收藏
页码：104 / 108
页数：5
相关论文
共 50 条
  • [41] Parallel solution-phase synthesis of substituted 2-(1,2,4-triazol-3-yl)benzimidazoles
    Ivanova, Natalya V.
    Sviridov, Sergey I.
    Stepanov, Aleksandr E.
    TETRAHEDRON LETTERS, 2006, 47 (46) : 8025 - 8027
  • [42] An efficient method for solution-phase parallel synthesis of 2-quinoxalinol salen schiff-base ligands
    Wu, Xianghong
    Gorden, Anne E. V.
    JOURNAL OF COMBINATORIAL CHEMISTRY, 2007, 9 (04): : 601 - 608
  • [43] A solution-phase parallel synthesis of 2-amino-5-furfurylidene-4H-imidazolin-4-ones
    Ding, MW
    Yang, SJ
    Sun, Y
    Liu, ZJ
    Liu, XP
    HETEROCYCLIC COMMUNICATIONS, 2002, 8 (05) : 493 - 496
  • [44] Synthesis of 2-arylbenzoxazoles via DDQ promoted oxidative cyclization of phenolic Schiff bases - a solution-phase strategy for library synthesis
    Chang, JB
    Zhao, K
    Pan, SF
    TETRAHEDRON LETTERS, 2002, 43 (06) : 951 - 954
  • [45] Parallel solution-phase synthesis of (Z)-3-(arylamino)-2,3-dehydroalanine derivatives and solid-phase synthesis of fused pyrimidones
    Cebasek, P
    Wagger, J
    Bevk, D
    Jakse, R
    Svete, J
    Stanovnik, B
    JOURNAL OF COMBINATORIAL CHEMISTRY, 2004, 6 (03): : 356 - 362
  • [46] Parallel Solution-phase Synthesis of (2S,4E)-4-(Arylaminomethylidene)pyroglutamic Acids
    Svete, Jurij
    Groselj, Uros
    Baskovc, Jernej
    Dahmann, Georg
    Stanovnik, Branko
    ZEITSCHRIFT FUR NATURFORSCHUNG SECTION B-A JOURNAL OF CHEMICAL SCIENCES, 2010, 65 (07): : 811 - 820
  • [47] Solution-phase parallel synthesis of novel 1,2,3,4-tetrahydroisoquinolin-1-ones as anticonvulsant agents
    Gitto, Rosaria
    Francica, Eleonora
    De Sarro, Giovambattista
    Scicchitano, Francesca
    Chimirri, Alba
    CHEMICAL & PHARMACEUTICAL BULLETIN, 2008, 56 (02) : 181 - 184
  • [48] Solution-phase parallel synthesis of a library of 1,4,6-trisubstituted-1H-pyrazolo[3,4-d]pyrimidines.
    Baindur, N
    Chadha, N
    Player, M
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2003, 225 : U225 - U225
  • [49] Solution-phase parallel synthesis of a 1,2,7-trialkyl-1H-imidazo[4,5-g]quinoxalin-6-ol library scaffold
    Zhang, J
    Zhang, L
    Zhang, SD
    Wang, YH
    Liu, G
    JOURNAL OF COMBINATORIAL CHEMISTRY, 2005, 7 (05): : 657 - 664
  • [50] Diversity by Divergence: Solution-Phase Parallel Synthesis of a Library of N-Diversified 1-Oxa-7-Azaspiro[4.5]clecan-2-yl-Propanes and -Butanes
    Kumar, Sarvesh
    Thornton, Paul D.
    Santini, Conrad
    ACS COMBINATORIAL SCIENCE, 2013, 15 (11) : 564 - 571
12345