Molecular Formula | C16H22ClN5O2 |
Molar Mass | 351.83118 |
Melting Point | 206-208° |
Solubility | DMSO (Slightly), Methanol (Slightly), Water (Slightly) |
Appearance | Solid |
Color | White to Pale Beige |
Storage Condition | under inert gas (nitrogen or Argon) at 2-8°C |
In vitro study | Alizapride has an N-allyl moiety, N-deallyl and/or epoxidation reactions may occur, and chemically reactive metabolites are expected to form. |
In vivo study | Alizapride is not toxic in mice and rats (especially in parenteral administration). Alizapride is mainly excreted as unmodified drug after oral or parenteral administration; However, about 25% of Alizapride undergoes metabolic transformation before it is excreted. In rats, alizapril (5 mg/kg, I. V.) antagonized the abovementioned dose of Apomorphine-induced reduction in gastrointestinal motility. |
CN200710042059.7
application date:
2007-06-15
Public/Announcement Number:
CN101066968B
Public/announcement date:
2012.11.07
applicant (patent):
Shanghai Bosu Pharmaceutical Technology Co., Ltd.
inventor:
Zhang Guangming , Sun Leda , Shen Xiao-wen
National and provincial code:
CN310104
Abstract:
The present invention relates to a preparation method of aripiprazole hydrochloride, comprising the steps of:(1) preparation of intermediate 2-methoxy-4-amino-5-nitrobenzoic acid;(2) preparation of intermediate 2-methoxy-4-acetamido-5-nitrobenzoic acid sodium salt;(3) preparation of intermediate 2-methoxy-4, 5-diaminobenzoic acid;(4) preparation of intermediate 5-methoxy-6-carboxybenzotriazole;(5) preparation of intermediate 5-methoxy-6-methoxycarbonylbenzotriazole;(6) preparation of aripiprazole hydrochloride. The invention has the advantages of high yield, simple operation and less pollution.