- CASPOFUNGIN ANALOG AND APPLICATIONS THEREOF
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Disclosed are a caspofungin analog and applications thereof. Said caspofungin analog is a compound having a structure as indicated in Formula (4), or pharmaceutically acceptable slats thereof. R1 can be chosen from hydroxyl, benzyloxy, phenoxy, substituted phenoxy, or substituted benzyloxy. R 2 , R 3 , R 4 , R 5 can be chosen from hydrogen, C1-C6 alkyl, C1-C6 alkoxy, hydroxyl, benzyloxyphenyl, substituted benzyloxyphenyl, nitro, fluorine, chlorine, bromine, or iodine. Also disclosed are a preparation method for and applications of said compound.
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- PROCESS FOR PREPARATION OF CASPOFUNGIN ACETATE AND INTERMEDIATES
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The present invention discloses a process for the preparation of Caspofungin and its intermediates from Pneumocandin B0.
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Page/Page column
(2014/02/15)
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- PROCESS FOR PREPARING CASPOFUNGIN AND NOVEL INTERMEDIATES THEREOF
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The present invention relates to a novel process for preparing the aza cyclohexapeptide compound 1-[(4R,5S)-5-[(2-aminoethyl)amino]-N2-(10,12-dimethyl-1-oxotetradecyl)-4-hydroxy-L-ornithine]-5-[(3R)-3-hydroxy-L-ornithine]-pneumocandin B0 (caspofungin), which can improve the problem due to a pungent odor and toxicity during the process and can prepare caspofungin as a final product at high yield compared to conventional processes, and to novel intermediates which are used in the preparation process.
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- Process for preparation of Caspofungin acetate
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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 thi
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Page/Page column 5
(2010/07/08)
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- Caspofungin free of caspofungin Co
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The present invention provides Caspofungin and salts thereof substantially free of Caspofungin C0 and salts thereof. The present invention also provides processes for the preparation of said Caspofungin and salts thereof and processes for the d
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Page/Page column 9-10
(2009/12/05)
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- Process for preparing pharmaceutical compound and intermediates thereof
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The present invention relates to novel intermediates of formula VII, or an acid addition salt or a solvate thereof, wherein R1 is —(CO)NH2, —CH2NH2 or —CN; R2═R3═H or R2 and Rsu
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Page/Page column 9
(2009/12/27)
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- Process and intermediates for the synthesis of caspofungin.
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The present invention relates to processes for preparing certain aza cyclohexapeptide compounds, e.g. caspofungin, novel intermediates used in said processes and a process for preparing said intermediates. In particular, the intermediates have the following formula, wherein X is amino, substituted amino or ether, and contain a cyano (nitrile) functionality.
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- Synthesis of the antifungal β-1,3-glucan synthase inhibitor CANCIDAS (caspofungin acetate) from pneumocandin B0
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A novel three-step synthesis of the highly functionalized antifungal agent CANCIDAS (caspofungin acetate, 2) is described, starting from the natural product pneumocandin B0 (1). The highlights of the synthesis include a stereoselective formatio
- Leonard Jr., William R.,Belyk, Kevin M.,Conlon, David A.,Bender, Dean R.,DiMichele, Lisa M.,Liu, Ji,Hughes, David L.
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p. 2335 - 2343
(2007/10/03)
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