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Volumn 15, Issue 2, 2011, Pages 382-388

Scale-up synthesis of a TRPV1 antagonist featuring a facile thiazolo[5,4-d]pyrimidine formation

Author keywords

[No Author keywords available]

Indexed keywords

AMINOPYRIMIDINES; LARGE SCALE PREPARATION; PYRIMIDINE RING; SCALE-UP; SYNTHESIS FEATURES;

EID: 79952831874     PISSN: 10836160     EISSN: 1520586X     Source Type: Journal    
DOI: 10.1021/op1002984     Document Type: Article
Times cited : (8)

References (27)
  • 9
    • 0036924776 scopus 로고    scopus 로고
    • Process Mass Intensity (PMI) is defined as the total mass of raw materials input divided by the mass of final Active Pharmaceutical Ingredient (API) output. It is adopted by the ACS Green Chemistry Institute as one of the benchmarks to measure the environmental impact and sustainability of chemical processes. For a review of PMI and other similar benchmarks, see: Constable, D. J. C.; Curzons, A. D.; Cunningham, V. L. Green Chem. 2002, 4, 521
    • (2002) Green Chem. , vol.4 , pp. 521
    • Constable, D.J.C.1    Curzons, A.D.2    Cunningham, V.L.3
  • 10
    • 0002306931 scopus 로고
    • 2O, 80 °C, 2 h, 100% yield. See Yousif, N. M. Tetrahedron 1989, 45, 4599
    • (1989) Tetrahedron , vol.45 , pp. 4599
    • Yousif, N.M.1
  • 12
    • 84986516402 scopus 로고
    • To the best of our knowledge, such couplings have only been reported with 2,3-dihalo-quinoxaline and quinones. See Katritzky, A. R.; Fan, W. Q. J. Heterocycl. Chem. 1988, 25, 901
    • (1988) J. Heterocycl. Chem. , vol.25 , pp. 901
    • Katritzky, A.R.1    Fan, W.Q.2
  • 26
    • 79952851861 scopus 로고    scopus 로고
    • See Supporting Information for more details.
    • See Supporting Information for more details.
  • 27
    • 79952852079 scopus 로고    scopus 로고
    • The isolated product was found to contain ∼0.5 equiv of HCl based on elemental analysis. See Experimental Section for details.
    • The isolated product was found to contain ∼0.5 equiv of HCl based on elemental analysis. See Experimental Section for details.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.