Solid phase synthesis of 5-aminopyrazoles and derivatives

Tetrahedron Letters

Volumn 38, Issue 52, 1997, Pages 9065-9068

  Watson, Stephen P ^a   Wilson, Richard D ^a   Judd, Duncan B ^a   Richards, Stephen A ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

HYDRAZINE DERIVATIVE; PYRAZOLE DERIVATIVE;

ARTICLE; CONTROLLED STUDY; DRUG SYNTHESIS;

EID: 0030733375     PISSN: 00404039     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0040-4039(97)10436-1     Document Type: Article

References (10)

1. For excellent recent reviews of the combinatorial libraries/chemistry area see; Terret, N.K.; Gardner, M.; Gordon, D.W.; Kobylecki, R.J.; Steele, J. Tetrahedron Report Number 377,. and Balkenhol, F.;von dem Bussche-Hunnefeld, C.; Lansky, A. and Zechel, C. Angew. Chem. Int. Ed. Engl. 1996, 35, 2288
2. For excellent recent reviews of the combinatorial libraries/chemistry area see; Terret, N.K.; Gardner, M.; Gordon, D.W.; Kobylecki, R.J.; Steele, J. Tetrahedron Report Number 377,. and Balkenhol, F.;von dem Bussche-Hunnefeld, C.; Lansky, A. and Zechel, C. Angew. Chem. Int. Ed. Engl. 1996, 35, 2288
3. For a review of the chemistry of β-ketonitriles see; Elnagdi, M.H.; El-Moghayar, M.R.H. and Elgemeie, G.E.H., Synthesis,1984, 1
4. See for example; Elnagdi, M.H.; El-Moghayar, M.R.H. and Fleita, D.H., Tetrahedron, 1974, 31, 63
5. Marzinzik, A.L. and Felder, E.R. Tet. Lett, 1996, 37,1003
6. Plunkett, M.J. and Ellman, J.A. J. Amer. Chem. Soc., 1995, 117, 3306
7. The Alkylation is accompanied by a number of side reactions (e.g. C-alkylation) which precludes direct alkylation of 6 with a resin supported alkylating agent
8. Hewlett Packard HP1050 HPLC system, 3μm Supelcosil column, UV detection at 280nm
9. VG Autospec Mass Spectrometer operating in positive electrospray mode, 8000 resolution.
10. Hewlett Packard HP1050 HPLC system, 10cm, 3μm hypersil BDS column coupled to a VG Platform Mass spectrometer operating in positive electrospray mode.