Reaktion #318249

Reaktionsgleichung

theophylline

triethylamine

pyrrolidine

→

7-(1-pyrrolidinyl)methyltheophylline

Ausbeute 72.0%

Lösungsmittel

tetrahydrofuran

Reaktionsbedingungen

Aufarbeitung

1. 1
   workup.WAITto equilibrate with 2 equivalents of 37% aqueous H2C=O for a few minutes until a solution
2. 2
   Sonstigewas obtained
3. 3
   EinengenThe solution was then concentrated in vacuo at <40°
4. 4
   SonstigeThe residue was triturated with ether
5. 5
   Filtrationthe suspension filtered
6. 6
   SonstigeThe residue from the suspension was dried

Vorschrift

Equivalent amounts of theophylline and triethylamine were allowed to equilibrate with 2 equivalents of 37% aqueous H2C=O for a few minutes until a solution was obtained. Then, 2 equivalents of pyrrolidine was added and the mixture was diluted with tetrahydrofuran and allowed to stir at room temperature overnight. The solution was then concentrated in vacuo at <40°. The residue was triturated with ether and the suspension filtered. The residue from the suspension was dried to give the desired 7-(1-pyrrolidinyl)methyltheophylline in 72% yield; mp 105°-108°, lit mp 108° (J. Org. Chem. 24, 562 (1959); NMR, UV and TLC consistent with the desired product.

Quelle