反应 #2286361

ord-52c8cb6a277d4a57ae29ab00b9eb36b2

反应方程式

CC(=O)OI1(OC(C)=O)(OC(C)=O)OC(=O)c2ccccc21
1,1,1-tri acetoxy-1,1-dihydro-1,2-benziodoxol-3(1H)-one
CC(C)(C)OC(=O)N1CCC(c2nc(C(O)CCc3ccccc3)cs2)CC1
tert-butyl 4-[4-(1-hydroxy-3-phenylpropyl)-1,3-thiazol-2-yl]piperidine-1-carboxylate
CC(C)(C)OC(=O)N1CCC(c2nc(C(=O)CCc3ccccc3)cs2)CC1
tert-Butyl 4-[4-(3-phenylpropanoyl)-1,3-thiazol-2-yl]piperidine-1-carboxylate

反应条件

详细条件
See reaction.notes.procedure_details.

后处理

  1. 1
    workup.ADDITION5 g of silica gel were then added
  2. 2
    其他the solvent was removed under reduced pressure
  3. 3
    其他The residue was purified chromatographically

实验过程

At room temperature, 1,1,1-tri acetoxy-1,1-dihydro-1,2-benziodoxol-3(1H)-one (15% strength solution in dichloromethane, 8.3 g) was added dropwise to a solution of tert-butyl 4-[4-(1-hydroxy-3-phenylpropyl)-1,3-thiazol-2-yl]piperidine-1-carboxylate (790 mg) in dichloromethane (7.9 ml). The reaction mixture was stirred at room temperature overnight. 5 g of silica gel were then added, and the solvent was removed under reduced pressure. The residue was purified chromatographically. This gave tert-butyl 4-[4-(3-phenylpropanoyl)-1,3-thiazol-2-yl]piperidine-1-carboxylate (545 mg).

来源

DOI: 10.6084/m9.figshare.5104873.v1专利: US09357779B2uspto-grants-2016_06