반응 #582495

ord-f6305112997b4ff8b60cc896053f3cee

반응 방정식

CCN(CC)CC
Et3N
CS(C)=O
DMSO
O=C(Cl)C(=O)Cl
oxalyl chloride
C[C@@H](CO)N(Cc1ccccc1)Cc1ccccc1
40
C[C@@H](CO)N(Cc1ccccc1)Cc1ccccc1
(S)-2-(N,N-Dibenzylamino)-1-propanol
C[C@@H](C=O)N(Cc1ccccc1)Cc1ccccc1
yellow oil
수율 98.0%
C[C@@H](C=O)N(Cc1ccccc1)Cc1ccccc1
(S)-2-(N,N-Dibenzylamino)propionaldehyde
수율 98.0%

반응 조건

상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    workup.WAITAfter 30 minutes
  2. 2
    추출The solution was extracted with satd
  3. 3
    추출NaHCO3 (20 mL) and the aqueous layer was extracted with CH2Cl2 (2×15 mL)
  4. 4
    세척The organic layer was washed with satd
  5. 5
    건조NaCl solution, dried with MgSO4
  6. 6
    농축an concentrated in vacuo at rt

실험 절차

Dry DMSO (0.53 mL, 7.43 mmol) was added to a stirred solution of oxalyl chloride (0.31 mL, 3.6 mmol) in CH2Cl2 (7.5 mL) at −78° C. The solution was allowed to stir 15 minutes followed by the addition of 40 (740 mg, 2.90 mmol) in CH2Cl2 (7.5 mL). After 30 minutes, Et3N (1.0 mL, 7.2 mmol) was added and allowed to warm to rt. The solution was extracted with satd. NaHCO3 (20 mL) and the aqueous layer was extracted with CH2Cl2 (2×15 mL). The organic layer was washed with satd. NaCl solution, dried with MgSO4 an concentrated in vacuo at rt to give 720 mg (98% yield) of a yellow oil which became a solid when cooled to −20° C. The aldehyde was used without further purification: mp 52-54° C. Lit. mp 55.5° C.; [α]26D=−36.0 (c 1,CHCl3 Lit. [α]20D=−35.1 (c 1, EtOAc); 1H NMR (400 MHz, CDCl3) δ 1.19 (d, 2H, J=7.0 Hz), 3.34 (q, 1H, J=7.0 Hz), 3.58 (d, 2H, J=13.7 Hz), 3.74 (d, 2H, J=13.7 Hz), 7.26 (m, 2H), 7.33 (m, H), 7.42 (m,4H), 9.74 (s, 1H); 13C NMR (100 MHz) δ 6.7, 54.9, 62.8, 3.3, 4.4, 4.8, 139.1, 204.6; FABMS m/z 408.2 (M+MB), 254.2 (M+H), 22.2 (M—CHO); HRFABMS calcd for C17H20NO Mr 254.1545 (M+H), found Mr254.1545. See, Dix et al., Arch Pharm (Weinheim) 1995, 328, 203-205.

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: USRE038793E1uspto-grants-2005_09