Process for preparing bosutinib
A preparation process, the technology of bosutinib, applied in the chemical and pharmaceutical field, can solve the problems of harshness, increase the reaction route, and low yield, and achieve the effect of short route, high yield and mild cyclization conditions
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[0016] Example 1
[0017] The preparation process of Bosutinib includes the following steps: taking 4-hydroxy-3-methoxybenzoic acid as a raw material and reacting with methanol to form an ester to obtain methyl 4-hydroxy-3-methoxybenzoate; Hydroxy-3-methoxybenzoic acid methyl ester is reacted with 1-bromo-3-chloropropane to obtain 4-(3-chloropropoxy)-3-methoxybenzoic acid methyl ester after alkylation; 4 The molar ratio of methyl-hydroxy-3-methoxybenzoate to 1-bromo-3-chloropropane is 1:1, and the reaction temperature is 50°C; 4-(3-chloropropoxy)-3-methoxy After nitration of methyl benzoate, methyl 4-(3-chloropropoxy)-5-methoxy-2-nitrobenzoate, 4-(3-chloropropoxy)-3-methoxy The molar ratio of methyl benzoate to fuming nitric acid is 1:1, and the reaction temperature is 40℃; methyl 4-(3-chloropropoxy)-5-methoxy-2-nitrobenzoate is obtained by reduction 4-(3-chloropropoxy)-5-methoxy-2-aminobenzoic acid methyl ester, the reducing agent used is iron powder, zinc powder or palladium ...
Example Embodiment
[0018] Example 2
[0019] The preparation process of Bosutinib includes the following steps: taking 4-hydroxy-3-methoxybenzoic acid as a raw material and reacting with methanol to form an ester to obtain methyl 4-hydroxy-3-methoxybenzoate; Hydroxy-3-methoxybenzoic acid methyl ester is reacted with 1-bromo-3-chloropropane to obtain 4-(3-chloropropoxy)-3-methoxybenzoic acid methyl ester after alkylation; 4 The molar ratio of methyl -hydroxy-3-methoxybenzoate to 1-bromo-3-chloropropane is 1:3, and the reaction temperature is 80°C; 4-(3-chloropropoxy)-3-methoxy After nitration of methyl benzoate, methyl 4-(3-chloropropoxy)-5-methoxy-2-nitrobenzoate, 4-(3-chloropropoxy)-3-methoxy The molar ratio of methyl benzoate to fuming nitric acid is 1:2, and the reaction temperature is 60℃; methyl 4-(3-chloropropoxy)-5-methoxy-2-nitrobenzoate is obtained by reduction 4-(3-chloropropoxy)-5-methoxy-2-aminobenzoic acid methyl ester, the reducing agent used is iron powder, zinc powder or palladium...
Example Embodiment
[0020] Example 3
[0021] The preparation process of Bosutinib includes the following steps: taking 4-hydroxy-3-methoxybenzoic acid as a raw material and reacting with methanol to form an ester to obtain methyl 4-hydroxy-3-methoxybenzoate; Hydroxy-3-methoxybenzoic acid methyl ester is reacted with 1-bromo-3-chloropropane to obtain 4-(3-chloropropoxy)-3-methoxybenzoic acid methyl ester after alkylation; 4 The molar ratio of methyl -hydroxy-3-methoxybenzoate to 1-bromo-3-chloropropane is 1:5, and the reaction temperature is 110°C; 4-(3-chloropropoxy)-3-methoxy After nitration of methyl benzoate, methyl 4-(3-chloropropoxy)-5-methoxy-2-nitrobenzoate, 4-(3-chloropropoxy)-3-methoxy The molar ratio of methyl benzoate to fuming nitric acid is 1:3, and the reaction temperature is 80°C; methyl 4-(3-chloropropoxy)-5-methoxy-2-nitrobenzoate is obtained by reduction 4-(3-chloropropoxy)-5-methoxy-2-aminobenzoic acid methyl ester, the reducing agent used is iron powder, zinc powder or palladi...
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