反应 #312608

ord-34dc52177d7e4b9b837d853360c2c0c0

反应方程式

O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)cccc21
1-(phenylsulfonyl)-4-piperzin-1-yl-1H-indole
CSC1=NCCN1.I
2-methylthio-2-imidazoline hydroiodide
CCN(C(C)C)C(C)C
N,N-diisopropylethylamine
O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(C4=NCCN4)CC3)cccc21
title product
O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(C4=NCCN4)CC3)cccc21
4-[4-(4,5-Dihydro-1H-imidazol-2-yl)-piperazin-1-yl]-1-(phenylsulfonyl)-1H-indole

溶剂

反应条件

温度
50°CELSIUS
详细条件
See reaction.notes.procedure_details.

后处理

  1. 1
    温度, cooled
  2. 2
    浓缩concentrated in vacuo
  3. 3
    其他to give a residue
  4. 4
    其他The residue is purified by HPLC

实验过程

A solution of 1-(phenylsulfonyl)-4-piperzin-1-yl-1H-indole (71 mg, 0.18 mmol) in dioxane is treated with 2-methylthio-2-imidazoline hydroiodide (52.7 mg, 0.22 mmol) and N,N-diisopropylethylamine (62 μl, 0.36 mmol), heated at 50° C. for 16 hr., cooled and concentrated in vacuo to give a residue. The residue is purified by HPLC to give the title product, 15 mg, identified by HPLC and mass spectral analyses (2.57 min; 410 M+H) using the LCMS conditions described in Table I.

来源

DOI: 10.6084/m9.figshare.5104873.v1专利: US07557098B2uspto-grants-2009_07