反应 #75450

ord-bc20141c7e094b3d8c1c83c7c79da1dd

反应方程式

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

反应物

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

试剂

无

溶剂

CO.O
water methanol

反应条件

详细条件
See reaction.notes.procedure_details.

后处理

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

实验过程

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).

来源

DOI: 10.6084/m9.figshare.5104873.v1专利: US06699503B1uspto-grants-2004_03