반응 #1994288

ord-c611585e6cb949fb9b4a8fbf877abd07

반응 방정식

CC(C)OB1OC(C)(C)C(C)(C)O1
2-isopropoxy-4,4,5,5-tetramethyl[1,3,2]dioxaborolane
C[CH](C)[Mg][Cl]
isopropylmagnesium chloride
Fc1cc(Cl)c(Cl)cc1Br
1-Bromo-4,5-dichloro-2-fluorobenzene
CCOCC
diethyl ether
CC1(C)OB(c2cc(Cl)c(Cl)cc2F)OC1(C)C
title compound
수율 71.1%
CC1(C)OB(c2cc(Cl)c(Cl)cc2F)OC1(C)C
2-(4,5-Dichloro-2-fluorophenyl)-4,4,5,5-tetramethyl-[1,3,2]dioxaborolane
수율 71.1%

반응 조건

온도
-10°CELSIUS
상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    온도to warm toward 0° C. for 1 hour
  2. 2
    온도cooled to −10° C. again
  3. 3
    온도to warm to ambient temperature
  4. 4
    추출extracted with 1N sodium hydroxide
  5. 5
    추출extracted with dichloromethane twice
  6. 6
    기타dried
  7. 7
    여과filtered
  8. 8
    농축concentrated

실험 절차

1-Bromo-4,5-dichloro-2-fluorobenzene (1.0 g, 4.11 mmol) was dissolved in tetrahydrofuran (THF; 20 mL) and cooled to −10° C. A 2.0M solution of isopropylmagnesium chloride (2.3 mL, 4.6 mmol) in THF was added dropwise via a syringe. The reaction mixture was stirred at −10° C. for 1 hour, allowed to warm toward 0° C. for 1 hour, then cooled to −10° C. again. A solution of 2-isopropoxy-4,4,5,5-tetramethyl[1,3,2]dioxaborolane (0.85 g, 4.56 mmol) in THF (1.0 mL) was then added dropwise and the reaction was allowed to warm to ambient temperature. The reaction mixture was then added to diethyl ether and extracted with 1N sodium hydroxide. The aqueous phases were combined, acidified to pH 3 with concentrated HCl, and extracted with dichloromethane twice. The organic phases were combined, dried, filtered and concentrated to give the title compound (0.85 g, 71% yield) that was used without further purification: 1H NMR (CDCl3): δ 7.73 (d, 1H), 7.12 (d, 1H), 1.3 (s, 12H).

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US08598085B2uspto-grants-2013_12