(2S,4S)-(-)-N-BOC-4-Diphenylphosphino-2-diphenylphosphinomethyl-pyrrolidine → Mitiglinide
反応式
CC(OC(N1[C@H](CP(C2C=CC=CC=2)C2C=CC=CC=2)C[C@H](P(C2C=CC=CC=2)C2C=CC=CC=2)C1)=O)(C)C.[CH:40](=[C:47]([CH2:51][C:52]([N:54]1[CH2:62][C@H:61]2[C@H:56]([CH2:57][CH2:58][CH2:59][CH2:60]2)[CH2:55]1)=[O:53])[C:48]([OH:50])=[O:49])[C:41]1[CH:46]=[CH:45][CH:44]=[CH:43][CH:42]=1>>[CH:44]1[CH:43]=[CH:42][C:41]([CH2:40][C@H:47]([C:48]([OH:50])=[O:49])[CH2:51][C:52]([N:54]2[CH2:55][C@H:56]3[C@H:61]([CH2:60][CH2:59][CH2:58][CH2:57]3)[CH2:62]2)=[O:53])=[CH:46][CH:45]=1参加物
3
実験手順
The preparation was carried out in the same manner as in Example 1, except that 2.92 mg of BPPM was used instead of 3.02 mg of PCPPM of Example 1. After the reaction, the residual ratio of 2-benzylidene-3-(cis-hexahydro-2-isoindolinylcarbonyl)propionic acid was 10.85%, and the optical purity of mitiglinide thus obtained was 96.1% e.e.
後処理
- customAfter the reaction