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.