Caspofungin analog and applications thereof
AssigneeShangham Tech-Well Biopharmaceutical Co., Ltd
InventorsBingming He, Ming Li, Zhijun Tang, Xiaoming Ji
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Abstract
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. R2, R3, R4, R5 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.
Claims21
A compound of Formula 4 or the pharmaceutically acceptable salts thereof,
- wherein R1 is selected from hydroxy, benzyloxy, phenoxy, substituted phenoxy, or substituted benzyloxy;
- R2, R3, R4, R5 is selected from hydrogen, C1-C6 alkyl, C1-C6 alkoxy, hydroxyl, benzyloxyphenyl, substituted benzyloxyphenyl, nitro, fluorine, chlorine, bromine, or iodine, respectively.
A preparation method for the compound of Formula 1, wherein said method comprises the following steps:
- mixing the compound of Formula 4 with ethylenediamine to obtain the compound of Formula 1.
A preparation method for the compound of Formula 1, wherein said method comprises the following steps:
- (a) mixing the compound of Formula 2 with strong leaving-group compound 5, thereby obtaining the compound of Formula 3;
- (b) mixing the compound of Formula 3 with a hydroxyl protectant, and then with a borane complex to obtain the compound of Formula 4;
- and
- (c) mixing the compound of Formula 4 with ethylenediamine to obtain the compound of Formula 1.
Dependencies are inferred from the claim text.