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US 2017/0247352 A1Published application
Method for preparing alectinib
AssigneeSuzhou Miracpharma Technolpgy Co., Ltd.
InventorXuenong Xu
Life of this patent
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Abstract
A method for preparing Alectinib (Alectinib, I), comprising the preparation steps: subjecting 6-cyano-1H-indole-3-carboxylate and 4-ethyl-3-(4-morpholine-4-yl-piperidine-1-yl)-α,α-dimethylbenzyl alcohol to condensation, hydrolyzing and cyclization reaction so as to prepare Alectinib (I). The preparation method has easily available raw materials and a simple process, and is economical and environmentally friendly and suitable for industrial production.
Claims10
A preparation method for Alectinib (Alectinib, I),
- the preparation steps comprising:
- using 6-cyano-1H-indole-3-carboxylic acid methyl ester or 6-cyano-1H-indole-3-carboxylic acid ethyl ester (II) to go through condensation reactions with 4-ethyl-3-(4-morpholin-4-yl-piperidin-1-yl)-α,α-dimethylphenylcarbinol (III) under the actions of catalysts to obtain 6-cyano-2-[2-[4-ethyl-3-(4-morpholin-4-yl-piperidin-1-yl)phenyl/propane-2-yl]-1H-indole-3-carboxylic acid methyl ester or 6-cyano-2-[2-[4-ethyl-3-(4-morpholin-4-yl -piperidin-1-yl)phenyl]propane-2-yl]-1H-indole-3-carboxylic acid ethyl ester (IV) respectively;
- then using 6-cyano-2-[2-[4-ethyl-3-(4-morpholin propane-2-yl]-1H-indole-3-carboxylic acid methyl ester or 6-cyano-2-[2-[4-ethyl -3-(4-morpholin-4-yl-piperidin-1-yl)phenyl]propane-2-yl]-1H-indole-3-carboxylic acid ethyl ester (IV) to go through hydrolysis reaction to obtain 6-cyano-2-[2-[4-ethyl-3-(4-morpholin-4-yl-piperidin-1-yl)phenyl/propane-2-yl]-1H-indole-3-carboxylic acid (V);
- and
- using 6-cyano-2-[2-[4-ethyl-3-(4-morpholin-4-yl-piperidin-1-yl) phenyl]propane-2-yl]-1H-indole-3-carboxylic acid (V) to go through cyclization reaction under the action of alkali accelerant to obtain Alectinib (I).
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