Diphenylmethane diisocyanate → Bromocriptine

HRID 729201Notes

Reaction equation

HRID 729201 reaction equation
C1C(CC2C=CC(N=C=O)=CC=2)=CC=C(N=C=O)C=1.[CH3:20][CH:21]([CH2:23][C@@H:24]1[N:33]2[C:34]([C@@:36]([NH:41][C:42]([C@@H:44]3[CH:60]=[C:59]4[C@@H:47]([CH2:48][C:49]5[C:50]6[C:51]4=[CH:52][CH:53]=[CH:54][C:55]=6[NH:56][C:57]=5[Br:58])[N:46]([CH3:61])[CH2:45]3)=[O:43])([CH:38]([CH3:40])[CH3:39])[O:37][C@@:32]2([OH:62])[C@H:31]2[N:27]([CH2:28][CH2:29][CH2:30]2)[C:25]1=[O:26])=[O:35])[CH3:22].CS(O)(=O)=O>>[CH3:22][CH:21]([CH2:23][C@@H:24]1[N:33]2[C:34]([C@@:36]([NH:41][C:42]([C@@H:44]3[CH:60]=[C:59]4[C@@H:47]([CH2:48][C:49]5[C:50]6[C:51]4=[CH:52][CH:53]=[CH:54][C:55]=6[NH:56][C:57]=5[Br:58])[N:46]([CH3:61])[CH2:45]3)=[O:43])([CH:38]([CH3:39])[CH3:40])[O:37][C@@:32]2([OH:62])[C@H:31]2[N:27]([CH2:28][CH2:29][CH2:30]2)[C:25]1=[O:26])=[O:35])[CH3:20]

Participants

3

Reactant 2

HCID 7570Diphenylmethane diisocyanateHCID 31100Bromocriptine mesylate

Product 1

HCID 31101Bromocriptine

Procedure

The formulations were tested on an Andersen™ cascade impactor to determine their aerodynamic particle properties. The cascade impactor was operated at 28.3 I/min and fitted with a USP induction port (<USP 601> Pharmacopeial Previews 22, 3065 (1995)). The particle size distributions were fractionated into mass of drug deposited on the pMDI actuator, USP induction port, eight stages and terminal filter. Five shots were actuated per test, with an interval of at least 30 seconds between shots to prevent cooling of the can and resultant moisture condensation. The bromocriptine content in each sample was determined by HPLC. The percentage of the total dose deposited from stage 4 to the terminal filter (corresponding to particles of MMAD less than 3.3 μm) was considered to be the fine particle fraction.

Workup

  1. customfitted with a USP induction port (<USP 601> Pharmacopeial Previews 22, 3065 (1995))
  2. filtrationfilter
  3. customwere actuated per test, with an interval of at least 30 seconds between shots
  4. temperatureto prevent cooling of the can
  5. customresultant moisture condensation
  6. filtrationfilter (corresponding to particles of MMAD less than 3.3 μm)

Sources & evidence

ORD record
ord-105bc92990b24b3d9a6b481443a8c1a0
Source dataset
uspto-grants-2009_09
Patent number
US07582284B2

Reaction notes

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