发明名称 |
PROCESS FOR PRODUCING SQUALAMINE |
摘要 |
PURPOSE: A process for producing squalamine is provided, thereby the squalamine can be cheaply and simply produced due to the use of cheap 3-keto-bisnocholenol as an initial compound. CONSTITUTION: The process for producing squalamine of formula(1) comprises the steps of: protecting a 3-keto group of 3-keto-bisnocholenol of formula(2) with an ethylenekital group and converting primary alcohol at C22 into an aldehyde group to produce 3-ethylenekital-23,24-bisnochola-5-en-22-al of formula(3); aldol condensing the compound of formula(3) to produce inone compound, hydrogenating the inone compound in the presence of platinum catalyst to produce 3-ethylenekital-cholest-5-en-24-on of formula(4); allyl oxidizing the compound of formula(4) to produce 3-ethylenekital-cholest-5-en-7,24-dion; selectively reducing double bond of the compound of formula(5) at C5 to produce 5alpha-cholestan and stereo selectively reducing a kito group at C7 and treating it with hydrochloric acid to produce 3-kito-5-alpha-cholestan-7,24-diol of formula(6); protecting hydroxy at C24 of the compound of formula(6) with t-butyldimethylsilyl, and converting kito at C3 to 3alpha-amino to produce 3alpha-amino-7,24-dihydroxycholest-5-en of formula(7); reacting the compound of formula(7) with polyamine aldehyde of formula(8) to produce a compound of formula(9); and treating the compound of formula(9) with acid to remove silly and a carbamate protecting group and to insert sulfone into the C24 site.
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申请公布号 |
KR100255031(B1) |
申请公布日期 |
2000.02.09 |
申请号 |
KR19980006425 |
申请日期 |
1998.02.27 |
申请人 |
KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY |
发明人 |
CHOI, BO SEUNG;CHOI, WON JUN;KIM, HONG SEOK;KIM, YONG JU;KWAK, HYEON JEONG;LEE, CHEOL HAE;LEE, SANG OK;SONG, JI SEOP |
分类号 |
(IPC1-7):C07J11/20 |
主分类号 |
(IPC1-7):C07J11/20 |
代理机构 |
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代理人 |
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主权项 |
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