发明名称 |
PROCESS FOR THE MANUFACTURE OF CYCLOPROPYLAMINE |
摘要 |
A modified novel process for preparing cyclopropylamine from gamma -butyrolactone is described. The gamma -butyrolactone ring is cleaved with a hydrohalide in the presence of a novel catalyst comprising an aqueous sulfuric acid solution. The 4-chlorobutyric acid, thus formed is converted into a hindered chlorobutyrate ester. The hindered ester based on secondary and tertiary alkanols of eight or less carbon atoms, is cyclized to form the hindered cyclopropanecarboxylate ester by a novel reaction medium consisting of solid caustic in a water-immiscible solvent and a phase transfer catalyst. The hindered cyclopropanecarboxylate ester is ammoniated to form cyclopropanecarboxamide by a novel catalyst comprising an alkali metal salt of a polyol having hydroxy groups on adjacent carbons. The carboxamide formed in substantially quantitative yields is converted to cyclopropylamine by a modified Hofmann reaction utilizing continuous degradation of the intermediate with simultaneous distillation. |
申请公布号 |
DE3665303(D1) |
申请公布日期 |
1989.10.05 |
申请号 |
DE19863665303 |
申请日期 |
1986.06.04 |
申请人 |
CIBA-GEIGY AG |
发明人 |
BLACKWELL, JOSEPH THOMAS;DAUGHETY, HAROLD LENN;GRACE, HENRY CLANTON;OLIVER, WARD HOPKINS |
分类号 |
C07C209/62;A61K;C07C51/083;C07C53/19;C07C67/00;C07C67/08;C07C67/317;C07C69/63;C07C69/74;C07C69/743;C07C209/00;C07C209/56;C07C211/35;C07C231/02;C07C233/58;C07D;(IPC1-7):C07C87/34;C07C85/00;C07C103/19 |
主分类号 |
C07C209/62 |
代理机构 |
|
代理人 |
|
主权项 |
|
地址 |
|