تفاعل #1244277

ord-ed4abaafdc3f41e5a5c5b294c4bc9051

معادلة التفاعل

O
water
[N-]=[N+]=NC(CO)CO
23
[N-]=[N+]=NC(CO)CO
2-Azidopropane-1,3-diol
COC(OC)(OC)c1ccccc1
(trimethoxymethyl)benzene
[N-]=[N+]=NC(CO)COC(=O)c1ccccc1
monoacylated product 27
المردود 93.0%
[N-]=[N+]=NC(CO)COC(=O)c1ccccc1
2-Azido-3-hydroxypropyl benzoate
المردود 93.0%

المذيبات

ظروف التفاعل

الظروف التفصيلية
See reaction.notes.procedure_details.

المعالجة

  1. 1
    تركيزconcentrated in vacuo
  2. 2
    أخرىPurification of the residue by silica gel flash chromatography

الإجراء التجريبي

Neat 23 (1.48 g, 12.65 mmol) was dissolved in CH2Cl2 (127 mL) and treated with a catalytic amount of p-toluene sulfonic acid monohydrate (0.048 g, 20 μmol) and (trimethoxymethyl)benzene (3.26 mL, 18.98 mmol) in CH2Cl2 at room temperature for 1 hr. After the formation of the orthoester was complete, a stoichiometric amount of water (340 μL, 18.98 mmol) was added to the mixture. The mixture was then stirred for 40 min and concentrated in vacuo. Purification of the residue by silica gel flash chromatography using 25% EtOAc/hexanes gave 2.6 g of monoacylated product 27 (93% yield) as a clear, colorless oil. 1H NMR (CDCl3, 400 MHz) δ: 8.03-8.06 (m, 2H), 7.58 (tt, J=1.6, 2.0, 1.6 1H), 7.43-7.47 (m, 2H), 4.54 (dd, J=4.4, 12.0 Hz, 1H), 4.46 (dd, J=6.8, 12.0 Hz, 1H), 3.85-3.91 (m, 1H), 3.80 (dd, J=4.8, 11.6 Hz, 1H), 3.73 (dd, J=6.0, 11.6 Hz, 1H).

المصدر

DOI: 10.6084/m9.figshare.5104873.v1براءة الاختراع: US07807394B2uspto-grants-2010_10