反应 #1880994

ord-574b524d424143dd97c48a1e553e053c

反应方程式

CCCn1c(=O)nc(SC)c2[nH]c(C34CCC(O)(CC3)CC4)nc21
8-(4-Hydroxy-bicyclo[2.2.2]oct-1-yl)-6-methylsulfanyl-3-propyl-3,7-dihydro-purin-2-one
CC[C@@H](N)CO
amino alcohol
CC[C@@H](N)CO
(R)-2-amino-1-butanol
CC[C@@H](N)CO
compound 2
CC[C@@H](N)CO
(R)-2-amino-1-butanol
CCCn1c(=O)nc(NC(CC)CO)c2[nH]c(C34CCC(O)(CC3)CC4)nc21
titled compound
CCCn1c(=O)nc(NC(CC)CO)c2[nH]c(C34CCC(O)(CC3)CC4)nc21
8-(4-Hydroxy-bicyclo[2.2.2]oct-1-yl)-6-(1-hydroxymethyl-propylamino)-3-propyl-3,7-dihydro-purin-2-one

溶剂

反应条件

温度
150°CELSIUS
详细条件
See reaction.notes.procedure_details.

后处理

  1. 1
    其他The resulting reaction mixture
  2. 2
    温度It was then cooled to rt
  3. 3
    其他purified by preparative HPLC

实验过程

8-(4-Hydroxy-bicyclo[2.2.2]oct-1-yl)-6-methylsulfanyl-3-propyl-3,7-dihydro-purin-2-one (125 mg, 0.36 mmol) was dissolved in 3 mL of DMSO along with an excess of an appropriate amino alcohol (e.g., (R)-(−)-2-amino-1-butanol (0.24 mL, 7 eq) for compound 2). The resulting reaction mixture was stirred at 150° C. for 3 h. It was then cooled to rt and purified by preparative HPLC to afford 110 mg of the titled compound.

来源

DOI: 10.6084/m9.figshare.5104873.v1专利: US07022686B2uspto-grants-2006_04