Reaction #75450

ord-bc20141c7e094b3d8c1c83c7c79da1dd

Reaction equation

COC(=O)C1=C(C)NC(C)=C(C(=O)O[C@H]2CCN(Cc3ccccc3)C2)[C@H]1c1cccc([N+](=O)[O-])c1.Cl
Barnidipine hydrochloride
→
COC(=O)C1=C(C)NC(C)=C(C(=O)O[C@H]2CCN(Cc3ccccc3)C2)[C@H]1c1cccc([N+](=O)[O-])c1
barnidipine HCl

Reactants

COC(=O)C1=C(C)NC(C)=C(C(=O)O[C@H]2CCN(Cc3ccccc3)C2)[C@H]1c1cccc([N+](=O)[O-])c1.Cl
Barnidipine hydrochloride

Reagents

None

Solvents

CO.O
water methanol

Conditions

Detailed conditions
See reaction.notes.procedure_details.

Workup

  1. 1
    workup.ADDITIONSeparately, PEG20000 and POLYOX303 were mixed
  2. 2
    OtherThe granules thus prepared
  3. 3
    Otherwere dried
  4. 4
    workup.ADDITIONafter addition of lubricant

Procedure

Barnidipine hydrochloride, TC-5E and HCO-40 were dissolved in water-methanol (1:9). Separately, PEG20000 and POLYOX303 were mixed. Using a fluidized-bed granulator, the latter mixture was sprayed with the above solution. The granules thus prepared were dried, and after addition of lubricant, the composition was compression-molded to provide tablets each measuring 9.0 mm in diameter and 300 mg (barnidipine HCl content: 15 mg).

Source

DOI: 10.6084/m9.figshare.5104873.v1Patent: US06699503B1uspto-grants-2004_03