反应 #42607

ord-4a032367bbd647bf9b5da8cedcc1a131

反应方程式

O=C1CCC(=O)O1
succinic anhydride
CCc1cccc(C2(NCC(O)C(N)Cc3cc(F)cc(F)c3)CC2)c1
3-Amino-4-(3,5-difluoro-phenyl)-1-[1-(3-ethyl-phenyl)-cyclopropylamino]-butan-2-ol
CCc1cccc(C2(NC[C@@H](O)[C@H](Cc3cc(F)cc(F)c3)NC(=O)CCC(=O)O)CC2)c1
4-[((1S,2R)-1-(3,5-difluorobenzyl)-3-{[1-(3-ethylphenyl)cyclopropyl]amino}-2-hydroxypropyl)amino]-4-oxobutanoic acid

反应条件

详细条件
See reaction.notes.procedure_details.

后处理

  1. 1
    workup.ADDITIONTo this solution was added
  2. 2
    workup.STIRRINGwas stirred overnight at 50° C
  3. 3
    其他The next morning reaction mixture
  4. 4
    浓缩was concentrated in vacuo
  5. 5
    其他yielding the product

实验过程

To a solution of 3-Amino-4-(3,5-difluoro-phenyl)-1-[1-(3-ethyl-phenyl)-cyclopropylamino]-butan-2-ol (0.500 g, 1.387 mmol) in chloroform (7 ml) was added TEA (0.58 ml, 4.161 mmol) with stirring under nitrogen for 30 min. To this solution was added succinic anhydride (0.138 g, 1.387 mmol) and reaction was stirred overnight at 50° C. The next morning reaction mixture was concentrated in vacuo, yielding the product. (ES+: 461.2)

来源

DOI: 10.6084/m9.figshare.5104873.v1专利: US07727997B2uspto-grants-2010_06