A new reagent and its polymer-supported variant for the amidination of amines

被引:26
作者
Dräger, G
Solodenko, W
Messinger, J
Schön, U
Kirschning, A
机构
[1] Univ Hannover, Inst Organ Chem, D-30167 Hannover, Germany
[2] Solvay Pharmaceut GMBH, D-30173 Hannover, Germany
关键词
D O I
10.1016/S0040-4039(01)02403-0
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
New reagents tor the high yielding amidination of primary and secondary amines are described. By attaching a benzyl substituent to the 3,5-dimethyl-1H-pyrazole-1-carboxamidine ring. a reagent 1 is obtained which allows easy work-up after amidination because of solubility of byproducts in organic solvents. In addition. the polystyrene-bound analogue 2 was prepared which allows amidination of various amines with high purity. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1401 / 1403
页数:3
相关论文
共 15 条
  • [1] 1H-PYRAZOLE-1-CARBOXAMIDINE HYDROCHLORIDE - AN ATTRACTIVE REAGENT FOR GUANYLATION OF AMINES AND ITS APPLICATION TO PEPTIDE-SYNTHESIS
    BERNATOWICZ, MS
    WU, YL
    MATSUEDA, GR
    [J]. JOURNAL OF ORGANIC CHEMISTRY, 1992, 57 (08) : 2497 - 2502
  • [2] Solid-phase synthesis of N,N′ substituted guanidines
    Dodd, DS
    Wallace, OB
    [J]. TETRAHEDRON LETTERS, 1998, 39 (32) : 5701 - 5704
  • [3] Gomez L, 2000, CHEM-EUR J, V6, P4016, DOI 10.1002/1521-3765(20001103)6:21<4016::AID-CHEM4016>3.0.CO
  • [4] 2-W
  • [5] GREENHILL JL, 1993, PROGR MED CHEM, V30, pCH5
  • [6] HANNON CL, 1993, BIOORGANIC CHEM FRON, V3, P192
  • [7] Solid-phase synthesis of disubstituted guanidines
    Kearney, PC
    Fernandez, M
    Flygare, JA
    [J]. TETRAHEDRON LETTERS, 1998, 39 (18) : 2663 - 2666
  • [8] Solid-phase synthesis of substituted guanidines using a novel acid labile linker
    Pátek, M
    Smrcina, M
    Nakanishi, E
    Izawa, H
    [J]. JOURNAL OF COMBINATORIAL CHEMISTRY, 2000, 2 (04): : 370 - 377
  • [9] Solid phase synthesis of guanidines
    Robinson, S
    Roskamp, EJ
    [J]. TETRAHEDRON, 1997, 53 (19) : 6697 - 6705
  • [10] ONE-POT C-ARYLMETHYLATION OF ACTIVE METHYLENE-COMPOUNDS WITH AROMATIC-ALDEHYDES INDUCED BY A ME3SICL-NAI-MECN REAGENT
    SAKAI, T
    MIYATA, K
    TSUBOI, SD
    UTAKA, MN
    [J]. BULLETIN OF THE CHEMICAL SOCIETY OF JAPAN, 1989, 62 (12) : 4072 - 4074