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US 2010/0168415 A1Published application
Process for preparation of Caspofungin acetate
OwnerKwang-Chung Lee, Yen-Shih Tung +1inventors
InventorsKwang-Chung Lee, Yen-Shih Tung, Hao-Ling Fang
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Abstract
A process for making caspofungin acetate comprising the steps of: A. selectively dehydrating pneumocandin Bo to obtain a nitrile; B. reducing the nitrile to primary amine; C. reacting the primary amine with an arylthiol in a suitable solvent to obtain a thioether; and D. reacting the thioether with ethylenediamine to obtain the caspofungin acetate having a formula as shown below:
Claims10
A process for preparation of Compound I, Caspofungin acetate, having a formula as shown below:
- the process comprising the steps of:
- A. Selectively dehydrating Pneumocandin Bo, Compound II, having a formula as shown below:
- with a dehydration agent to obtain a nitrile with the formula of Compound V as shown below:
- B. Reducing Compound V in the presence of a metal catalyst to obtain an amine with the formula of Compound III as shown below:
- C. Reacting Compound III with an arylthiol in the presence of a solvent to obtain Compound VI as shown below:
- and
- D. Reacting Compound VI with ethylenediamine in the presence of solvent or without solvent to obtain Caspofungin acetate of Compound I.
4 more elements
Dependencies are inferred from the claim text.