Preparation method for caspofungin
AssigneeShanghai Techwell Biopharmaceutical Co., Ltd.
InventorsBingming He, Ming Li, Zhijun Tang, Xiaoming Ji
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Abstract
Disclosed is a preparation method for caspofungin, comprising the steps: (a) a compound as represented in Formula 2 and a strong leaving group 5 are mixed to obtain a compound as represented in Formula 3; (b) the compound as represented in Formula 3 and ethylenediamine are mixed to obtain a compound as represented in Formula 4; and, (c) the compound as represented in Formula 4 is mixed with a hydroxyl protection agent, and then a borane complex is mixed in to obtain a compound as represented in Formula 1.
Claims16
A preparation method for the compound of Formula 1, wherein said method comprises the following steps:
- (a) mixing the compound of Formula 2 with a strong leaving-group compound 5, thereby obtaining the compound of Formula 3;
- (b) mixing the compound of Formula 3 with ethylenediamine to obtain the compound of Formula 4;
- and
- (c) mixing the compound of Formula 4 with a hydroxyl protectant, and then with a borane complex to obtain the compound of Formula 1;
- wherein in step (a), the strong leaving-group compound 5 is a sulphydryl-substituted aromatic ring compound, and wherein, in obtaining Formula 3, in the sulphydryl-substituted aromatic ring compound R1 is selected from hydroxy, benzyloxy, phenoxy, substituted phenoxy, or substituted benzyloxy, and R2, R3, R4 and R5 are selected from hydrogen, C1-C6 alkyl, C1-C6 alkoxy, hydroxyl, benzyloxyphenyl, substituted benzyloxyphenyl, nitro, fluorine, chlorine, bromine, or iodine.
Dependencies are inferred from the claim text.