Solid phase synthesis of 5-aminopyrazoles and derivatives part II

Tetrahedron Letters

Volumn 39, Issue 18, 1998, Pages 2827-2830

  Wilson, Richard D ^a,b   Watson, Stephen P ^a   Richards, Stephen A ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

^b Shire Canada   (Canada)

Author keywords

[No Author keywords available]

Indexed keywords

5 AMINOPYRAZOLE; NITRILE; PYRAZOLE DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; DRUG SCREENING; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG TARGETING; SOLID PHASE EXTRACTION;

EID: 0032580403     PISSN: 00404039     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0040-4039(98)00257-3     Document Type: Article

References (10)

1. 1 For recent reviews of solid phase organic synthesis see - Früchtel J.S., Jung G., Angew. Chem. Intl. Ed. Engl. 1996, 35, 17 and Hermkens P.H.H., Ottenheijm H.C.J., Rees D. Tetrahedron Report No. 394 Tetrahedron 1996, 52, 4527
2. 1 For recent reviews of solid phase organic synthesis see - Früchtel J.S., Jung G., Angew. Chem. Intl. Ed. Engl. 1996, 35, 17 and Hermkens P.H.H., Ottenheijm H.C.J., Rees D. Tetrahedron Report No. 394 Tetrahedron 1996, 52, 4527
3. 2 Watson S.P., Wilson R.D., Judd D.B., Richards S.A., Tetrahedron Letters 1997, 38, 9065
4. 3 Bredereck H., Effenberger F., Botsch H., Chem.Ber. 1964, 97, 3397
5. 4 Bailey N., Cooper A.W.J., Deal M.J., Dean A.W., Gore A.L., Hawes M.C., Judd D.B., Merritt A.T., Storer R., Travers S., Watson S.P. Chimia, 1997, 51, 832
6. 1H NMR spectrum of cleaved product in DMSO - d6 containing 5mM p-nitro phenol as an internal standard.
7. 6 Purities judged by lc/ms - Hewlett Packard HP1050 HPLC system, 10cm, 3μm hypersil BDS column coupled to a VG Platform Mass Spectrometer operating in positive electrospray mode.
8. 7 The resin is stored at the enamine stage, due to long term instability of the resin bound aldehyde.
9. 8 Hewlett Packard HP 1050 HPLC system, 3μm Supelcosil column, UV detection at 280nm.
10. 9 VG Autospec Mass Spectrometer operating in positive electrospray mode, 8000 resolution