تفاعل #59107

ord-7d9c37c55faf40e195d89965ec8334dc

المذيبات

ظروف التفاعل

الظروف التفصيلية
See reaction.notes.procedure_details.

المعالجة

  1. 1
    تركيزThe reaction concentrated
  2. 2
    workup.DISSOLUTIONthe resulting residue dissolved in EtOAc
  3. 3
    غسيلThe organic phase was washed with saturated aqueous NaHCO3 (3×)
  4. 4
    استخلاصthe combined aqueous portions were extracted with EtOAc
  5. 5
    تركيزThe combined organic portions were concentrated
  6. 6
    أخرىto give an orange residue as 2
  7. 7
    أخرىthe resulting reaction
  8. 8
    درجة الحرارةmaintained at rt for 14 h
  9. 9
    أخرىthe remaining solution was partitioned between EtOAc and water
  10. 10
    أخرىThe layers were separated
  11. 11
    استخلاصthe aqueous phase extracted with EtOAc (3×)
  12. 12
    تركيزThe combined organic layers were concentrated
  13. 13
    أخرىto give an orange solid as 3 which
  14. 14
    أخرىwas carried forward without further purification

الإجراء التجريبي

Ethyl chloroformate (2 eq.) was added to a stirring solution of aniline 1 (1 eq.) and iPr2NEt (2 eq.) in dry THF (14 mL) at 0° C. The reaction was allowed to warm to rt over 2 h. The reaction concentrated and the resulting residue dissolved in EtOAc. The organic phase was washed with saturated aqueous NaHCO3 (3×) and the combined aqueous portions were extracted with EtOAc. The combined organic portions were concentrated to give an orange residue as 2. The residue was dissolved in DMF (20 mL), hydrazine monohydrate (1 eq.) added and the resulting reaction maintained at rt for 14 h. The reaction volume was reduced and the remaining solution was partitioned between EtOAc and water. The layers were separated and the aqueous phase extracted with EtOAc (3×). The combined organic layers were concentrated to give an orange solid as 3 which was carried forward without further purification: LCMS m/z 333.3 (MH+), tR=2.29 min.

المصدر

DOI: 10.6084/m9.figshare.5104873.v1براءة الاختراع: US07423150B2uspto-grants-2008_09