Abstract: The present invention provides a blank liposome with ginsenoside Rg3 or its analog as the membrane material, preparations and uses thereof. The disclosed blank liposome has a membrane comprising a lipid and a ginsenoside analog of Formula I, presenting remarkable advantages in film formation, encapsulation efficiency, targeted drug delivery, blood circulation time, stability, safety and homogeneity. It can also be used to load active substances of drugs and cosmetics, biological agents, polynucleotides or oligonucleotides, and the preparation process is convenient.

Abstract: The present invention provides a blank liposome with ginsenoside Rg3 or its anaglog as the membrane material, preparations and uses thereof. The disclosed blank liposome has a membrane comprising a lipid and a ginsenoside analog of Formula I, presenting remarkable advantages in film formation, encapsulation efficiency, targeted drug delivery, blood circulation time, stability, safety and homogeneity. It can also be used to load active substances of drugs and cosmetics, biological agents, polynucleotides or oligonucleotides, and the preparation process is convenient.

Abstract: Among others, the present invention provides a blank liposome, preparation methods thereof, and a loaded liposome including the blank liposome and an active substance. The liposomes have a membrane comprising lipids and a ginsenoside of Formula I, and may further comprise a surfactant, a heat-sensitive excipient, a pH sensitive material, or an ion additive.

Abstract: Among others, the present invention provides a blank liposome, preparation methods thereof, and a loaded liposome including the blank liposome and an active substance. The liposomes have a membrane comprising lipids and a ginsenoside of Formula I, and may further comprise a surfactant, a heat-sensitive excipient, a pH sensitive material, or an ion additive.

Abstract: A saponin nano micelle, preparing method, application and pharmaceutical composition thereof is disclosed in the present invention. The saponin nano micelle comprises one or more of saponins represented by formula 1, in which, R1 and R2 are independently —H or a hydrophilic group, R3 is —H or —OH, R4 is a lipophilic group. The preparing method of the saponin nano micelle is that mixing the saponin with an organic solvent which can dissolve saponin, and then removing the organic solvent. The saponin micelle acts as a convey medium of the drug ingredients, and can replace conventional drug carriers such as pharmaceutical solubilizers or polymeric micelle, which has high safety and great significance. The pharmaceutical ingredients can prolong circulation time and biological half-life of drug in the blood, and increase the accumulation of drug in lesions, and reduce adverse reactions.

Abstract: A saponin nano micelle, preparing method, application and pharmaceutical composition thereof is disclosed in the present invention. The saponin nano micelle comprises one or more of saponins represented by formula 1, in which, R1 and R2 are independently —H or a hydrophilic group, R3 is —H or —OH, R4 is a lipophilic group. The preparing method of the saponin nano micelle is that mixing the saponin with an organic solvent which can dissolve saponin, and then removing the organic solvent. The saponin micelle acts as a convey medium of the drug ingredients, and can replace conventional drug carriers such as pharmaceutical solubilizers or polymeric micelle, which has high safety and great significance. The pharmaceutical ingredients can prolong circulation time and biological half-life of drug in the blood, and increase the accumulation of drug in lesions, and reduce adverse reactions.

Abstract: Described is a process for preparing docetaxel 1, including the following steps: a) hydroxyl acylation reaction of compound 2 and 3 to obtain compound 4; b) deprotection group R1 of the hydroxyl group of compound 4 obtained from step a to prepare compound 5; c) removing one tert-butoxycarbonyl of compound 5 obtained from step b to prepare compound 6; d) removing one acetyl of compound 6 obtained from step c to prepare compound 1; wherein, R1 represents tert-butyl dimethyl silyl, triethylsilyl, ethoxyethyl, tetrahydropyranyl, trichloroethoxycarbonyl or methoxymethyl, Boc is tert-butoxycarbonyl, Ac is acetyl, and Ph is phenyl. Also disclosed are intermediates of docetaxel and methods for preparation thereof.

Abstract: In the present invention, a synthesis method of Imatinib is disclosed, which comprises the following steps: the Imatinib, namely 4-(4-methyl-piperazin-1-ylmethyl)-N-[4-methyl-3-[4-(3-pyridinyl)-pyrimidin-2-ylamino]-benzami de shown in formula (III), is formed by reacting 4-methyl-N-3-(4-pyridin-3-yl-pyrimidin-2-yl)-1,3-benzenediamine shown in formula (I) with 4-(4-methyl-piperazin-1-methyl)-benzoic ester shown in formula (II), under the action of a base and in a non-protonic organic solvent, in the above generic chemical structural formula, R represents aliphatic alkyl having 1-10 carbon, phenyl, substituted phenyl, benzyl or substituted benzyl. The present invention provides a new synthesis method of Imatinib, which is formed under mild reaction conditions, and is environmentally friendly with a high-yield.

Abstract: In the present invention, a synthesis method of Imatinib is disclosed, which comprises the following steps: the Imatinib, namely 4-(4-methyl-piperazin-1-ylmethyl)-N-[4-methyl-3-[4-(3-pyridinyl)-pyrimidin-2-ylamino]-benzamide shown in formula (III), is formed by reacting 4-methyl-N-3-(4-pyridin-3-yl-pyrimidin-2-yl)-1,3-benzenediamine shown in formula (I) with 4-(4-methyl-piperazin-1-methyl)-benzoic ester shown in formula (II), under the action of a base and in a non-protonic organic solvent, in the above generic chemical structural formula, R represents aliphatic alkyl having 1-10 carbon, phenyl, substituted phenyl, benzyl or substituted benzyl. The present invention provides a new synthesis method of Imatinib, which is formed under mild reaction conditions, and is environmentally friendly with a high-yield.

Abstract: Disclosed herein is a process for preparation of imatinib free base which comprises condensing 4-Methyl-N-(4-pyridin-3-yl-pyrimidin-2-yl)-benzene-1,3-diamine with 4-(4-Methyl-piperazin-1-ylmethyl)-benzoic acid ester in the presence of base including organic bases and inorganic bases in an organic solvent to form imatinib.

Abstract: The present invention disclosed an process for preparing docetaxel 1, including the following steps: a) hydroxyl acylation reaction of compound 2 and 3 to obtain compound 4; b) deprotection group R1 of the hydroxyl group of compound 4 obtained from step a to prepare compound 5; c) removing one tert-butoxycarbonyl of compound 5 obtained from step b to prepare compound 6; d) removing one acetyl of compound 6 obtained from step c to prepare compound 1; wherein, R1 represents tert-butyl dimethyl silyl, triethylsilyl, ethoxyethyl, tetrahydropyranyl, trichloroethoxycarbonyl or methoxymethyl, Boc is tert-butoxycarbonyl, Ac is acetyl, and Ph is phenyl. The present invention also disclosed intermediates of docetaxel and methods for preparation thereof.