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Isolation of amorphous (2S)-N-[(2R)-1-[[(3S,6S,8S,12S,13R,16S,17R,20S,23S)-13-[(2S)-butan-2-yl]-12-hydroxy-20-[(4-methoxyphenyl)methyl]-6,17,21-trimethyl-3-(2-methylpropyl)-2,5,7,10,15, 19,22-heptaoxo-8-propan-2-yl-9,18-dioxa-1,4,14,21-tetrazabicyclo[21.3.0]hexacosan-16-yl]amino]-4-methyl-1-oxopentan-2-yl]-N-methyl-1-(2-oxopropanoyl)pyrrolidine-2-carboxamide

IP.com Disclosure Number: IPCOM000248540D
Publication Date: 2016-Dec-15
Document File: 3 page(s) / 243K

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The IP.com Prior Art Database

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Isolation of amorphous (2S)-N-[(2R)-1-[[(3S,6S,8S,12S,13R,16S,17R,20S,23S)-13-[(2S)-

butan-2-yl]-12-hydroxy-20-[(4-methoxyphenyl)methyl]-6,17,21-trimethyl-3-(2-

methylpropyl)-2,5,7,10,15, 19,22-heptaoxo-8-propan-2-yl-9,18-dioxa-1,4,14,21-

tetrazabicyclo[21.3.0]hexacosan-16-yl]amino]-4-methyl-1-oxopentan-2-yl]-N-methyl-1-(2-

oxopropanoyl)pyrrolidine-2-carboxamide

(2S)-N-[(2R)-1-[[(3S,6S,8S,12S,13R,16S,17R,20S,23S)-13-[(2S)-butan-2-yl]-12-hydroxy-20-

[(4-methoxyphenyl)methyl]-6,17,21-trimethyl-3-(2-methylpropyl)-2,5,7,10,15,19,22-hepta-

oxo-8-propan-2-yl-9,18-dioxa-1,4,14,21-tetrazabicyclo[21.3.0]hexacosan-16-yl]amino]-4-

methyl-1-oxopentan-2-yl]-N-methyl-1-(2-oxopropanoyl)pyrrolidine-2-carboxamide

(Compound I) has the following chemical structure:

Chemical Formula: C57H87N7O15

Exact Mass: 1109.63

Molecular Weight: 1110.36

It is a cyclic depsipeptide isolated from the marine tunicate Aplidium albicans.

Compound I displays a broad spectrum of antitumor activities.

Amorphous Compound I was isolated using precipitation and filtration or evaporation

from solution under reduced pressure as described herein below.

Fig.1 XRD pattern of amorphous Compound I

Experimental

X-Ray powder diffraction:

BRUKER D8 Advance X-ray powder diffractometer, CuKα radiation (λ = 1.5406 Å);

Lynxeye XE detector, low amount PMMA sample holder with zero background plate was

used. Prior to analysis, the dry samples were gently ground by means of mortar and pestle in

order to obtain a fine powder. The ground...